| DC45818 |
LPM4870108 |
LPM4870108 is a potent and orally active pan-Trk (WT and MT) inhibitor, with IC50s of 0.2 nM, 2.4 nM, 3.5 nM and 2.3 nM for TrkC, TrkA, TrkAG595R and TrkAG667C, respectively. LPM4870108 shows selectivity for Trk over ALK (IC50=182 nM). LPM4870108 exhibits anti-tumor activity. |
|
| DC45824 |
iHCK-37 |
iHCK-37 (ASN05260065) is a potent and specific Hck inhibitor with a Ki value of 0.22 μM. iHCK-37 blocks HIV-1 viral replication with an EC50 value of 12.9 μM. iHCK-37 is used for chronic myeloid leukemia (CML) research. |
|
| DC45832 |
Epitinib succinate |
Epitinib succinate is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib succinate can be used for the research of cancer. |
|
| DC46051 |
Zanubrutinib D5 |
Zanubrutinib D5 (BGB-3111 D5) is deuterium labeled Zanubrutinib. Zanubrutinib is a selective Bruton tyrosine kinase (Btk) inhibitor. |
|
| DC46126 |
Axitinib-d3 |
Axitinib-d3 (AG-013736-d3) is deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively. |
|
| DC46163 |
Epitinib |
Epitinib is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib can be used for the research of cancer. |
|
| DC46170 |
EGFR-IN-16 |
EGFR-IN-16 (compound 3) is a potent EGFR inhibitor with pIC50 of 4.85 and 4.74 for EGFR and HER-2, respectively. |
|
| DC46175 |
TIE-2/VEGFR-2 kinase-IN-2 |
TIE-2/VEGFR-2 kinase-IN-2 is a potent dual VEGFR2 and Tie-2 inhibitor with pIC50 values of 8.61 and 8.56, respectively. TIE-2/VEGFR-2 kinase-IN-2 is an anti-angiogenic agent and can be used for cancer research. |
|
| DC46183 |
TPX-0022(CSF1R-IN-2)
Featured
|
TPX-0022 (CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with enzymatic kinase inhibition IC50s of 0.14 nM, 0.71 nM and 0.12 nM, respectively. TPX-0022 modulates the tumor immune microenvironment in preclinical models. |
|
| DC57050 |
DZD9008
Featured
|
DZD9008 is an oral, potent, irreversible, wild type-selective EGFR TKI against EGFR or HER2 Exon20ins and other mutations. |
|
| DC46219 |
EGFR mutant-IN-1 |
EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFRL858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFRWT (IC50 >1.0 μM). |
|
| DC46369 |
GSK215
Featured
|
GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect. |
|
| DC46385 |
c-Fms-IN-9 |
c-Fms-IN-9 is a c-FMS inhibitor extracted from patent WO2014145023A1, Compound Example 7. c-Fms-IN-9 inhibits unphosphorylated c-FMS kinase (uFMS) and uKIT with IC50s of <0.01 μM and 0.1-1 μM, respectively. |
|
| DC46406 |
CHMFL-ABL-039 |
CHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor with the IC50s of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used in the research of chronic myeloid leukemia. |
|
| DC46418 |
CGP77675 hydrate |
CGP77675 hydrate is an orally active and potent inhibitor of Src family kinases. CGP77675 hydrate inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively),and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. Anticancer activity. |
|
| DC46434 |
JBJ-02-112-05 |
JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFRL858R/T790M. |
|
| DC46436 |
DYRK1-IN-1 |
DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe. |
|
| DC46437 |
VEGFR-3-IN-1 |
VEGFR-3-IN-1 is a potent and selective VEGFR3 inhibitor with an IC50 of 110.4 nM. VEGFR-3-IN-1 significantly inhibits proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells by inactivating the VEGFR3 signaling pathway, and also effectively inhibits breast cancer growth. |
|
| DC46449 |
FGFR1 inhibitor-2 |
FGFR1 inhibitor-2 is a FGFR1 inhibitor (IC50 is 4.55 μM in MDA-MB-231 cells). FGFR1 inhibitor-2 can be used for the research of metastatic triple-negative breast cancer. |
|
| DC46456 |
JNJ28871063 hydrochloride |
JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2. |
|
| DC46464 |
BGB-102 |
BGB-102 is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively. |
|
| DC46609 |
Cyclotraxin B TFA |
Cyclotraxin B TFA, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B TFA non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B TFA can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects. |
|
| DC46660 |
c-Fms-IN-7 |
c-Fms-IN-7 is a cFMS inhibitor extracted from patent WO2011079076A1, example159, has an IC50 of 18.5 nM. |
|
| DC46928 |
TL-895 |
TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor with an IC50 and a Ki of 1.5 nM and 11.9 nM, respectively. TL-895 is used be for JAKi-relapsed/refractory myelofibrosis, acute myeloid leukemia, COVID-19 and cancer research. |
|
| DC46929 |
Erlotinib-13C6 |
Erlotinib-13C6 (CP-358774-13C6) is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. |
|
| DC46930 |
Sunvozertinib |
Sunvozertinib is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC50s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52). |
|
| DC46931 |
Gunagratinib |
Gunagratinib (ICP-192) is a low toxicity and orally active pan-FGFR (fibroblast growth factor receptors) inhibitor that potently and selectively inhibits FGFR activities irreversibly by covalent binding. Gunagratinib can be used for the research of cancer. |
|
| DC46932 |
Luxeptinib |
Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells. |
|
| DC46933 |
Timtraxanib |
Timtraxanib (AVI-3207) is a selective VEGF-2 inhibitor. Timtraxanib can be used for the research of senile macular degeneration. |
|
| DC46934 |
(Rac)-SAR131675 |
(Rac)-SAR131675 is the racemate of SAR131675. SAR131675 is a potent and selective VEGFR3 inhibitor with an IC50 of 23 nM. |
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