(E/Z)-4-hydroxy Tamoxifen is an active metabolite of tamoxifen that is formed by the action of cytochrome P450 2D6 in human liver.

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A novel, potent and selective inhibitor of CDK4/6 with biochemical IC50 of 1 nM and 2 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively.

A novel, potent and selective inhibitor of CDK4/6 with biochemical IC50 of 1 nM and 2 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively.

AZD8186 is an inhibitor of the beta isoform of phosphoinositide-3 kinase (PI3K), with potential antineoplastic activity.

AZD8835 ia a novel mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity against PI3Kβ (IC50=431 nM) and PI3Kγ (IC50=90 nM).

AZD9496 is a potent and orally bioavailable selective estrogen receptor downregulator(Ki=0.7 nM) and antagonist.

BIIB021(CNF2024) is an orally available, fully synthetic small-molecule inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively.

BMS-599626 (AC480) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, respectively.

BMS-754807 is a potent and reversible inhibitor of IGF-1R/IR family kinases, inhibits IGF-1R, IR, Met, TrkA and TrkB with IC50 of 1.8 nM, 1.7 nM, 5.6 nM, 7.4 nM and 4.1 nM, respectively.

BSI-201 (Iniparib; NSC-746045) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC).

CI994 (Tacedinaline) is an anti-cancer drug which inhibits HDAC1 with IC50 of 0.57 μM.

CO-1686 hydrobromide is a novel, irreversible and orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M (IC50=21 nM).

Dofequidar fumarate(MS-209 fumarate), an orally active quinoline compound, has been reported to overcome MDR by inhibiting ABCB1/P-gp, ABCC1/MDR-associated protein 1, or both.

E7449 is an orally bioavailable, potent, small molecule inhibitor of PARP1 and PARP2; enhances the efficacy of radiotherapy and chemotherapy and has potent single agent anticancer activity in BRCA-deficient tumors.

Elacestrant dihydrochloride (RAD1901 dihydrochloride) is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.

Elacridar is an orally selectly potent P-glycoprotein (P-gp/ABCG1) inhibitor.

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.

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.

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

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-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-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.

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.

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

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

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.

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.

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.

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

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

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.

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.

Poziotinib, is an orally bioavailable, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with potential antineoplastic activity.

Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q).

SNG-1153 is a synthetic modulator of ER-α36

SU14813 is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), Kit, and fms-like tyrosine kinase 3 (FLT-3).

TAK-117(INK1117,MLN1117) is an orally bioavailable inhibitor of the class I phosphoinositide 3-kinase (PI3K) alpha isoform with potential antineoplastic activity.

Tariquidar (XR9576) is a potent and selective noncompetitive inhibitor of P-glycoprotein with Kd of 5.1 nM.

Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM, respectively.

Veliparib is a potent inhibitor of both PARP-1 and PARP-2 by [3H]NAD+ with Kis of 5.2 and 2.9 nmol/L, respectively.

Deforolimus(AP23573; MK-8669; Ridaforolimus) is a selective mTOR inhibitor with IC50 of 0.2 nM; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin. IC50 value: 0.2 nM [1] Target: mTOR in vitro: Treatment of HT

MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2.