Endoxifen is a Estrogen receptor α (ERα) ligand; potent antiestrogen,an active metabolite of the cancer drug tamoxifen.

Entinostat (MS-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM, compared with HDACs 4, 6, 8, and 10. Phase 1/2.

Entrectinib (RXDX-101), a potent and selective small molecule inhibitor of TrkA/B/C, ROS1, and ALK kinases, has demonstrated early clinical activity when orally administered intermittently under fasting conditions.

Enzastaurin (LY317615) is a potent PKCβ selective inhibitor with IC50 of 6 nM, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Phase 3.

EPZ011989 is a potent, orally-available EZH2 Inhibitor.

Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1-4 with IC50 values of 1.2, 2.5, 3.0 and 5.7nM, respectively.

Eribulin is an anticancer drug marketed by Eisai Co. under the trade name Halaven. Eribulin is also known as E7389 and ER-086526, and also carries the US NCI designation NSC-707389. It is used to treat certain patients with breast cancer and liposarcoma.

Eribulin Mesylate (E7389 Mesylate), a synthetic analogue of halichondrin B in phase III clinical trials for breast cancer, binds to tubulin and microtubules.

Erlotinib (OSI-744; NSC 718781; R1415) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

Erlotinib HCl is an HER1/EGFR inhibitor with IC50 of 2 nM.

ETC-159 is a potent and specific inhibitor of Wnt secretion. ETC-159 inhibits _beta_-catenin reporter activity in a dose-dependent manner with an IC50 of 2.9 nM.

Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM.

EW-7197 is a potent ALK5 inhibitor. EW-7197 showed potent in vivo anti-metastatic activity, indicating its potential for use as an anti-cancer therapy.

Fadrozole is a non-steroidal aromatase inhibitor (IC50s = 5 and 1.4 nM for human placental and rat ovarian microsomal aromatase, respectively).

FGF401 is an inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity.

Flavopiridol competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM, and CDK7 with IC50 of 300 nM.

Flavopiridol hydrochloride competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA.

FLT3/AXL inhibitor

Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.

Foretinib (GSK1363089; XL880; EXEL-2880; GSK089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM. Less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR.

Fosbretabulin disodium(CA 4DP; CA 4P) is a microtubule destabilizing drug, a type of vascular-targeting agent, a drug designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis.

Foslinanib (TRX-818) is an orally bioavailable agent with potential antineoplastic and anti-vasculogenic mimicry (VM) activities, induces cancer cell apoptosis and inhibits cancer cell proliferation.

Fruquintinib (HMPL-013) is a novel small molecule compound that selectively inhibits vascular endothelial growth factor receptors (VEGFRs).

G1T28(Trilaciclib) is a potential first-in-class, short-acting IV CDK4/6 inhibitor being developed to preserve hematopoietic stem cells and enhance immune system function during chemotherapy.

GDC-0077 is an orally available PI3K inhibitor with potential antineoplastic activity. GDC-0077 is extracted from patent WO 2017001645 A1, formula I.

GDC-0084 （RG7666）, is a phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity.

GDC0575（ARRY-575，RG7441）is a small molecule inhibitor of cell cycle checkpoint kinase 1 (Chk1), with potential chemosensitization activity.

GDC-0879 is a novel potent, selective B-Raf inhibitor for B-RafV600E with IC50 of 0.13 nM.

GDC-0941 2 MeSO3H salt is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

GDC-0941 is a potent inhibitor of PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ with IC50 of 3 nM, 33 nM, 3 nM and 75 nM, respectively.

GDC-0973 is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase, also known as MEK, a serine/threonine kinase that is a component of the RAS/RAF/MEK/ERK pathway.

GDC-0980 (RG7422) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM, respectively. Also a mTOR inhibitor with Ki of 17 nM, and highly selective versus others PIKK family kinases.

Gefitinib (Iressa, ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively.

Gemcitabine(Gemzar) belongs to the group of medicines called antimetabolites.

Gimeracil(Gimestat) is an inhibitor of dihydropyrimidine dehydrogenase (DPYD), which degrades pyrimidine including 5-fluorouracil in the blood; inhibits homologous recombination.

Glumetinib (SCC 244) is a novel potent and highly selective inhibitor of c-Met kinase with IC50 of 0.42 nM.

GSK 525762A is a potent small molecule inhibitors that disrupt the function of the BET family of bromodomains (Brd2, Brd3, and Brd4).

GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.

GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM; displays >100-fold selectivity against the closely related Aurora A-TPX2 complex(IC50=490 nM).

GSK2126458 is a highly selective and potent inhibitor of PI3K with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2 , respectively.

GSK2256098 is small molecule FAK kinase inhibitor.

GSK2879552 is an orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.

GSK3326595(EPZ015938) is the first-in-class protein arginine methyltransferase-5 (PRMT5) inhibitor.

GSK690693 is a pan-Akt inhibitor targeting Akt1, Akt2 and Akt3 with IC50 of 2 nM, 13 nM, and 9 nM, respectively.

GSK923295 is a first-in-class, specific allosteric inhibitor of CENP-E kinesin motor ATPase with Ki of 3.2 nM, and less potent to mutant I182 and T183.

H3B-6527 is an orally bioavailable inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity.

HMN-214(IVX214) is a potent PLK1 inhibitor an average IC50 of 0.12 μM.

IACS-010759 (IACS010759) is a small molecule inhibitor of mitochondrial oxidative phosphorylation (OXPHOS), targets complex I of the mitochondrial electron transport chain.

Iberdomide (CC-220) is a cereblon modulator in clinical development for systemic lupus erythematosis. Iberdomide exhibits an IC50 of 60 nM in TR-FRET cereblon binding assay.

ICEC0942 is a selective CDK7 inhibitor, with IC50s of 41 nM and 578 nM for CDK7/CycH/MAT1 and CDK2/cycE1, respectively.

ICG-001 is a small-molecule antagonist of b-catenin/TCF-mediated transcription (IC50 = 3 uM) and specifically downregulates the expression of a subset of b-catenin/TCF-responsive genes. ICG-001 binds specifically to cyclic AMP response element-binding pro

Idarubicin Hcl is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor.

IDH305 is an inhibitor of the citric acid cycle enzyme isocitrate dehydrogenase [NADP] cytoplasmic (isocitrate dehydrogenase 1; IDH1) with mutations at residue R132 (IDH1(R132)), with potential antineoplastic activity.

IDO-IN-1 is an indoleamine-2,3-dioxygenase (IDO) inhibitor with IC50 of 59 nM, shows activity in Hela cell (IC50=12 nM).

Ifosfamide is a nitrogen mustard alkylating agent used in the treatment of cancer.

Imatinib Mesylate is orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM, respectively.

Imisopasem manganese (M40403) is a stable non-peptidyl mimetic of manganese superoxide MnSOD.

INCB053914 (INCB-053914) is a novel potent, and selective ATP-competitive, pan-PIM kinase inhibitor with IC50 of 0.24/30.0/0.12 nM for PIM1/2/3, respectively.

INCB28060 is a novel orally active inhibitor (IC50=0.13 nM) of c-MET kinase.

INCB8761(PF-4136309) is a potent, Selective, and orally bioavailable CCR2 antagonist.

INK 128 is a potent and selective mTOR inhibitor with IC50 of 1 nM; >200-fold less potent to class I PI3K isoforms.

IPI-145 is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities.

IPI-549 is an orally administered immuno-oncology development candidate that selectively inhibits PI3K-gamma.

Ispinesib (SB 715992) is a potent mitotic kinesin KSP (Eg5) inhibitor with a Ki and an IC50 of 0.6 and 4.1 nM, respectively.

Itacitinib is a potent and selective inhibitor of JAK1, with >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis.

Ixabepilone (Azaepothilone B; BMS 247550) is an epothilone B analog and nontaxane microtubule-stabilizing compound with clinical activity in a range of solid tumors.

JNJ-26854165 (Serdemetan) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53.

JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases.

K 858 is an ATP-uncompetitive mitotic kinesin Eg5 inhibitor, which does not effect microtubule dynamics.

KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.

KO-947 is a small molecule inhibitor of extracellular-signal-regulated kinases 1 and 2 (ERK1/2), as a potential treatment for cancers in which the mitogen activated protein kinase (MAPK) pathway.

KP1019 (FFC14A) is just the second ruthenium-based anticancer agent after NAMI-A which was developed to the stage of clinical trials.

KPT-330, analog of KPT-185, is an orally bioavailable selective CRM1 inhibitor.

KRN633 is a potent and selective VEGFR inhibitor. which inhibits tyrosine phosphorylation of VEGFR-2 (IC50 = 1.16 nmol/L) in human umbilical vein endothelial cells.

KW 2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase.

KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1/2

KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

Lapatinib

Lapatinib Ditosylate (GW572016, GW2016, Tykerb, Tyverb) is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively.

Lapatinib ditosylate(GW-572016 ditosylate) is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively.

Lazertinib (YH25448, GNS-1480) is a highly potent, mutant-selective, irreversible, brain-penetrant and orally active EGFR tyrosine-kinase inhibitors for both the T790M mutation and activating EGFR mutations

LB-100 is a small-molecular protein phosphatase 2A(PP2A)inhibitor with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.

LGK-974 is a potent and specific PORCN inhibitor, and inhibits Wnt signaling with IC50 of 0.4 nM.

Lifirafenib（BGB-283） is a Novel potent and selective RAF Kinase and EGFR inhibitor.

LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.

LOXO-195 is a next-generation TRK kinase (TKI) inhibitor, with IC50s of 0.6±0.1 nM, <2.5 nM for TRKA and TRKC respectively.

ORY-1001 dihydrochloride (RG-6016, Ladademstat) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM, displays high selectivity for KDM1A over other FAD-containing monoamine oxidases.

LSZ102 is a potent, orally bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.

This product is discontinued. LTX-315 (Oncopore) is a synthetic 9-mer anticancer peptide that preferentially permeabilizes mitochondrial membranes, thereby causing partially BAX/BAK1-regulated, caspase-independent necrosis.

LX1606 is an orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity.

LXH254 is a potent CRAF inhibitor extracted from patent WO2018051306A1, Compound A. LXH254 also is a potent BRAF inhibitor.

LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM. Phase 2.

LY2228820 is a novel and potent p38MAPK inhibitor (the IC50 for p38αMAPK and p38βMAPK were 7 nM and 3 nM, respectively).

LY2510924 is an inhibitor of CXC chemokine receptor 4 (CXCR4), with potential antineoplastic activity.

LY-2584702 is an orally available inhibitor of p70S6K signaling; inhibits p70S6K and prevents phosphorylation of the S6 subunit of ribosomes.

LY2603618(IC-83) is a potent and selective small molecule inhibitor of Chk1 protein kinase activity in vitro (IC50=7 nM) and the first selective Chk1 inhibitor to enter clinical cancer trials.

LY2606368 2Hcl is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.

LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.

LY2784544 is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2.

LY2874455 is a novel and potent FGF/FGFR inhibitor.

LY2940680 binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling.

LY3009120 is a potent and selective pan-RAF inhibitor with potential anticancer activity.

LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.

LY3039478 a orally bioavailable, novel small molecule Notch inhibitor with an IC50 of ~1nM in most of the tumor cell lines tested.

LY3200882 is a novel, highly selective TGFβRI small molecule inhibitor.

LY3214996 is a selective and novel ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines.

LY3295668 is a potent, orally active and highly specific Aurora-A kinase inhibitor, with Ki values of 0.8 nM and 1038 nM for AurA and AurB, respectively.

LY335979 (Zosuquidar) is a potent modulator of P-glycoprotein-mediated multidrug resistance with Ki of 60 nM.

MAK683 is a novel PRC2/EED inhibitor.

Marimastat is a broad spectrum MMP inhibitor and selective TACE inhibitor

Masitinib is a broad coronavirus 3CL inhibitor that effectively blocks replication of SARS-CoV-2. Science 20 Jul 2021: eabg5827 DOI: 10.1126/science.abg5827

MDV3100 is an androgen-receptor (AR) antagonist with IC50 of 36 nM.

Melphalan(Sarcolysin; L-PAM) is a chemotherapy drug belonging to the class of nitrogen mustard alkylating agents; attaches the alkyl group to the guanine base of DNA.

Methazolastone (Temozolomide, Temodar, Temodal) is a DNA damage inducer.

Methoxsalen (Oxsoralen)

MGCD0103 (Mocetinostat) is a potent HDAC inhibitor with IC50 of 0.15, 0.29 and 1.66 μM for HDAC 1, HDAC 2 and HDAC 3, respectively.

MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-MLL interaction.

MI-77301 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

Mivebresib is a novel BET family inhibitor, disrupts critical transcription programs that drive prostate cancer growth to induce potent anti-tumor activity in vitro and in vivo.

MK-1775 is a potent and selective Wee1 inhibitor with IC50 of 5.2 nM.

MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2.

MK-2461 is a potent, multi-targeted inhibitor for c-Met(WT/mutants) with IC50 of 0.4-2.5 nM, less potent to Ron, Flt1; 8- to 30-fold greater selectivity of c-Met targets versus FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB.

MK-4101 is a potent SMO Inhibitor of the Hedgehog Pathway, highly active against Medulloblastoma and Basal Cell Carcinoma.

MK-4827 is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity.

MK-4827 is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity.

MK-4827(Niraparib) tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM; with great activity in cancer cells with mutant BRCA-1 and BRCA-2; >330-fold selective against PARP3, V-PARP and Tank1.

MK-5108 (VX-689) is a highly selective Aurora A inhibitor with IC50 of 0.064 nM; 220- and 190-fold more selective for Aurora A than Aurora B/C.

ML264 is a novel small molecule inhibitor of Krüppel-like factor 5 (KLF5).

ML385 is a novel and specific NRF2 inhibitor.

MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM.

MLN4924 is a small molecule inhibitor of Nedd8 activating enzyme (NAE) with IC50 of 4 nM.

MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM; exhibits more than 40-fold selective for Aurora A than Aurora B.

MLN-9708 is a proteasome inhibitor, which inhibits the activity of the proteasome, blocking the targeted proteolysis normally performed by the proteasome.

Motesanib (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more selective for VEGFR than PDGFR and Ret.

Motesanib is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is appr 10-fold more selective for VEGFR than PDGFR and Ret.

MPC-3100 is an orally bioavailable, synthetic, second-generation small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.

MPT0E028 is a potent HDAC inhibitor that inhibits nuclear HDAC activity with IC50 of 11.1 nM in HeLa cells, 9-30 times more potent than SAHA.

MRK003 is a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma.

N,N’N’-triethylenethiophosphoramide (ThioTEPA) is a cancer chemotherapeutic member of the alkylating agent group.

NAMI-A is a ruthenium anticancer agent and a metastasis inhibitor.

Napabucasin (BBI608) is an orally-administered small molecule which can block cancer stem cell (CSC) self-renewal and induces cell death in CSCs as well as non-stem cancer cells.

NCB-0846 is a novel,first-in-class,orally TNIK inhibitor with an IC50 value of 21 nM,that have shown strong anti-tumor efficacy against several cancer models.

Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor with IC50 of 59 nM and 92 nM for HER2 and EGFR, respectively.

Netazepide (YF476, Sograzepide) is a potent, selective and orally active gastrin/CCK-2 antagonist with IC50 of 0.1 nM.

Nilotinib (AMN-107, Tasigna) is a Bcr-Abl inhibitor with IC50 less than 30 nM.

Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM.

Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM.

NLG-8189 is an inhibitor of IDO and INDOL1 (IDO2)

NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor with excellent ADME and pharmacokinetic profiles and high efficacy in vivo.

NVP-AEW541 is a potent inhibitor of IGF-1R with IC50 of 86 nM.

NVP-BEP800 is a novel, fully synthetic HSP90β inhibitor with IC50 of 58 nM.

NVP-BGT226 is a novel dual PI3K/mTOR inhibitor with IC50 of 1 nM.

NVP-TAE684(TAE684) is a highly potent and selective small-molecule ALK inhibitor, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM.

ODM-201 is a potent and full antagonists for human AR (hAR) with IC50 values of 26 nM by transactivation assays in AR-HEK293 cells.

Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1 and PARP2 with IC50 of 5 nM and 1 nM, respectively.

Olutasidenib is a highly potent, selective inhibitor of mutant Isocitrate dehydrogenase (IDH)1 that could be used in the treatment of acute myeloid leukemia.

Ombrabulin (AVE8062) hydrochloride is a synthetic derivative of CA-4-P, which inhibits growth in a large number of drug-resistant animal tumors and carcinogen-induced tumors.

Ombrabulin (AVE8062) hydrochloride is a synthetic derivative of CA-4-P, which inhibits growth in a large number of drug-resistant animal tumors and carcinogen-induced tumors.

ONO-4059 is a highly selective, orally bioavailable BTK inhibitor with a potency (IC50) of 2.2 nM.

ONO-4059 is a novel Small Molecule Dual Inhibitor Of Bruton’s Tyrosine Kinase (Btk) and Tec Kinase.

Oprozomib (ONX 0912) selectively inhibits CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.

ORIC-101 (ORIC101) is a highly potent, selective steroidal glucocorticoid receptor (GR) antagonist (IC50=5.6 nM) with reduced androgen receptor (AR) agonistic activity.

OSI-027 is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, respectively.

OSI-906 (Linsitinib) is a selective inhibitor of IGF-1R and IR with IC50 of 35 nM and 75 nM, respectively.

OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl.

Ostarine (MK-2866) is a selective androgen receptor modulator (SARMs) that regulates cardiomyocyte function, improves bone healing, regulates uterine function, and influences muscle tissue metabolism.

OSU-03012(AR-12) is a potent inhibitor of recombinant PDK-1 with IC50 of 5 μM and 2-fold increase in potency over OSU-02067.

OTSSP167 is a highly potent MELK inhibitor (IC50 = 0.41 nM) and inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like).

OTSSP167 is a highly potent MELK inhibitor (IC50 = 0.41 nM) and inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like).

Oxaliplatin is a second generation potent platinum-based anti-neoplastic agent that is believed to form inter- and intrastrand DNA adducts which activate signaling pathways culminating in apoptosis. The development of Oxaliplatin was inspired from the eff

PAK4-IN-1 is an inhibitor of p21-activated kinases (PAKs), with IC50 of ≤100 nM in MTT assay.

Palbociclib (PD-0332991) is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity.

Palbociclib is an oral, small molecule cyclin-dependent kinase 4/6 (CDK4/6) inhibitor, now in Phase 3 clinical development for advanced breast cancer.

Panobinostat(LBH-589) is a broad-spectrum HDAC inhibitor; low nanomolar concentrations (IC50=5-20 nM) of LBH589 induced cell-cycle arrest, apoptosis, and histone (H3K9 and H4K8) hyperacetylation in MOLT-4 and Reh cell.

Pazopanib Hcl (GW-786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively.

Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR-α/β, and c-Kit.

PCI-32765 (Ibrutinib) is a potent and highly selective Btk inhibitor with IC50 of 0.5 nM.

PD0325901 (PD325901) is selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM.

Pelitinib (EKB-569; WAY-EKB 569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM.

Pemetrexed disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively.

Perifosine (KRX-0401) is a novel Akt inhibitor with IC50 of 4.7 μM.

PF 477736 is a CHK inhitor with Ki values of 0.49 and 47 nM for Chk1 and Chk2 respectively. A proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity

PF-00562271 is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively.

PF-03758309 is an orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity.

PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM, susceptible to oncogenic mutations (no activity to Y1230C mutant).

PF-04449913 is a potent and orally bioavailable inhibitor of smoothened with IC50 of 5 nM(Gli-luciferase reporter reporter in C3H10T1/2); the hedgehog pathway inhibitor

PF-06459988 (PF06459988, PF 6459988) is a potent, selective, irreversible EGFR mutants with IC50 of 13, 7, 21 and 90 nM for EGFR L858R-T790M, Del-T790M, L858R, and EGFR Del, respectively.

PF06463922 is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.

PF-06840003 is an orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1),with potential immunomodulating and antineoplastic activities.

PF-2341066 (Crizotinib) is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nnM, respectivley.

PF299804 is a potent, irreversible pan-ErbB inhibitor against ErbB1, ErbB2 and ErbB4 with IC50 of 6 nM, 45.7 nM and 73.7 nM, respectively.

PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively.

PFK-158 is a potent and selective inhibitor of PFKFB3 that is currently being investigated in a phase I study in patients with advanced solid malignancies.

PI3K-IN-2 is a PI3K inhibitor, inhibits pPKB and pS6 with "++++/+++(+)" in A2058 melanoma cell.

PIM447 is novel pan-PIM kinase inhibitor, including Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase.

PKC-412 is a broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms (α, β, γ), PDFRβ, VEGFR2, Syk, PKCη, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR. Displays potent antitumor activity.

PKI-587 is a highly potent dual PI3K/mTOR kinase inhibitor with IC50 of 0.4 nM and <0.1 μM for PI3K-α and mTOR, respectively.

Plerixafor is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.

PLX3397 is a tyrosine kinase inhibitor that potently inhibits the colony stimulating factor 1 (CSF1) receptor kinase, a driving force in the development and growth of PVNS.

PLX4032 (Vemurafenib, RG7204, Zelboraf, RO5185426) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM.