MAPK
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EGFR inhibitor
AV-412 is an EGFR/HER2 inhibitor that binds to and inhibits the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER2), which may result in the inhibition of tumor growth and angiogenesis.- Le Zhang, .et al. , Oncotarget, 2016, Apr 12; 7(15): 19948-19959 PMID: 26942566
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EGFR inhibitor
PF299804 is a potent, orally available, irreversible inhibitor of tyrosine kinase human epidermal growth factor receptors (HER) 1 (EGFR), HER2, and HER4.- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Hamzehlou S, .et al. , Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Momeny M, .et al. , Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
- Majid Momeny, .et al. , Sci Rep, 2017, 7: 4204 PMID: 28646172
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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PDGFR/FLT3 Inhibitor
Crenolanib (CP-868596) is an orally bioavailable, selective small molecule inhibitor of the PDGFR tyrosine kinase, inhibiting both PDGFRA and PDGFRB at picomolar concentrations.- N Naganna, .et al. , EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
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IGF-1R inhibitor
OSI-906 is a potential first-in-class selective small molecule, dual kinase inhibitor of both insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR).- Masao Kakoki, .et al. , Communications Biology, 2021, 4:775
- Nakamura T, .et al. , J Med Food, 2018, Jul;21(7):701-708 PMID: 29583066
- Tzeng SF, .et al. , FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Takata N, .et al. , In Vitro Cell Dev Biol Anim., 2016, May;52(5):607-15 PMID: 26956358
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IGF-1R inhibitor
BMS-536924 is an effective inhibitor of IGF-IR, causing a reversion of an IGF-IR - mediated transformed phenotype.- Qiao Zhou, .et al. , Onco Targets Ther, 2015, 8: 689-697 PMID: 25897243
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EGFR, HER2 and VEGFR inhibitor
XL647 is an orally bioavailable small-molecule RTK inhibitor that binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including EGFR, HER2, ERBB2, VEGFR and EphB4. -
IGF-1R inhibitor
BMS-754807 is an efficacious, orally active growth factor 1 receptor/insulin receptor family-targeted kinase inhibitor that may act in combination with a wide array of established anticancer agents.- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
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FGFR inhibitor
AZD4547 is a potent, selective and orally active pan-FGFR inhibitor, with IC50s of 0.2, 2.5, 1.8 and 165 nM for FGFR1, 2, 3 and 4, respectively.- Ryuma Tokunaga, .et al. , Oncotarget, 2016, Apr 12; 7(15): 19748-19761 PMID: 26933914
- Mitsuko Kawano, .et al. , Adv Radiat Oncol, 2016, Jul-Sep; 1(3): 170-181 PMID: 28740887
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JAK2/FLT3 inhibitor
TG-101348 is an orally bioavailable, ATP-competitive and selective inhibitor of Janus-associated kinase 2 with potential antineoplastic activity. -
c-Met inhibitor
ARQ-197 is a selective inhibitor of the c-Met receptor tyrosine kinase- Wang L, .et al. , J Am Chem Soc, 2019, Aug 14;141(32):12673-12681 PMID: 31381313
- Koide H, .et al. , Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
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c-MET Inhibitor
INCB28060, a novel inhibitor of c-MET kinase. INCB28060 exhibits picomolar enzymatic potency and is highly specific for c-MET with more than 10,000-fold selectivity over a large panel of human kinases. This inhibitor potently blocks c-MET phosphorylation and activation of its key downstream effectors in c-MET-dependent tumor cell lines.- Geoffrey A Pettitt, .et al. , J Pathol, 2023, Feb;259(2):220-232 PMID: 36385700
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EGFR inhibitor
ARRY334543 is a potent, orally active small molecule inhibitor of EGFR and ErbB-2.- Hamzehlou S, .et al. , Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
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FGFR Inhibitor
BGJ398 is a potent and selective inhibitor with potential antiangiogenic and antineoplastic activities of fibroblast growth factor receptor (FGFR) tyrosine kinases 1, 2, 3 and 4 (with IC50 values of 0.9, 1.4, 1.0 and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4 respectively).- Takehito Yamamoto, .et al. , Cancers (Basel), 2020, Jul 22;12(8):E2010 PMID: 32708005
- Daniel Limonta, .et al. , J Infect Dis, 2019, 2019 PMID: 30799482
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Anil Kumar, .et al. , Sci Rep, 2018, 8: 5477 PMID: 29615760
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IGF-1R Inhibitor
GSK1838705A is a small-molecule kinase inhibitor that inhibits IGF-IR and the insulin receptor with IC50s of 2.0 and 1.6 nmol/L, respectively.
- Watanabe S, .et al. , Pflugers Arch, 2016, Apr;468(4):667-77 PMID: 26577585
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EGFR Inhibitor
BMS 599626 is an orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases (IC50=22, 32 and 190 nM, respectively) with potential antineoplastic activity. -
HER2/EGFR inhibitor
TAK-285 is an investigational HER2/EGFR inhibitor that penetrates the CNS in Rats with an Intact Blood Brain Barrier (BBB). TAK-285 has inhibitory activity against HER2 and EGFR kinases with IC50 values for HER2 and EGFR of 17 nmol/L (95% CI 12-24) and 23 nmol/L (95% CI 18-30), respectively.[1] -
c-Met Inhibitor
EMD-1214063 is an inhibitor of MET tyrosine kinase with potential antineoplastic activity. It binds to MET tyrosine kinase and disrupts MET signal transduction pathways, which may induce apoptosis in tumor cells overexpressing this kinase. -
multi-kinase inhibitor
Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. -
VEGFR/EGFR Inhibitor
BMS-690514 is a potent and selective inhibitor of epidermal growth factor receptor (EGFR), HER2, and HER4, as well as the VEGF receptor kinases. -
multi-kinase inhibitor
Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively. -
Itk Inhibitor
The ITK inhibitor BMS-509744 disrupts several aspects of HIV replication.- Samson AA, .et al. , Methods Mol Biol, 2017, 1571:221-232 PMID: 28281259
- YK Tak, .et al. , Anal. Chem., 2013, 85 (9), pp 4273-4278 PMID: 23573871
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EGFR inhibitor
Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. -
multiple receptor tyrosine kinases inhibitor
Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.- Paula Sagmeister, .et al. , J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
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PDGFRα/β inhibitor
CP 673451 is a potent PDGFR-β inhibitor with an IC50 of 1 nM.- Kaori Aoto, .et al. , Oncotarget, 2018, Sep 25; 9(75): 34090-34102 PMID: 30344924
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c-Met/VEGFR-2 inhibitor
E7050 (also known as golvatinib is an orally bioavailable dual kinase inhibitor of c-Met (hepatocyte growth factor receptor) and VEGFR-2 (vascular endothelial growth factor receptor-2) tyrosine kinases with potential antineoplastic activity. -
IGF-1R Inhibitor
AG-1024 (Tyrphostin) is a specific inhibitor of insulin-like growth factor-1 (IGF-1) and insulin receptor tyrosine kinase activity. Exhibits lower IC50 values for IGF-1 than for the insulin receptor. Also inhibits insulin-stimulated cellular proliferation.- Maeda A, .et al. , Mol Nutr Food Res. , 2014, 58(6):1177-89 PMID: 24668740
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VEGFR inhibitor
Apatinib (YN968D1) is a tyrosine kinase inhibitor that selectively inhibits the vascular endothelial growth factor receptor-2 (VEGFR2, also known as KDR) that inhibits VEGF-mediated endothelial cell migration and proliferation thus blocking new blood vessel formation in tumor tissue.- Wonjin Park, .et al. , Biomed Pharmacother, 2021, Feb;134:111110 PMID: 33338749
- Majid Momeny, .et al. , Sci Rep, 2017, 7: 45954 PMID: 28383032
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RTK inhibitor
Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor, which inhibits Ba/F3 cells transformed to IL3 independence by ZNF198-FGFR1 or BCR-FGFR1 with IC50 values of 150 nM and 90 nM, respectively.- Yunping Hu, .et al. , Cancer Lett, 2022, Oct 28;547:215867 PMID: 35985510
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EGFR inhibitor
Erlotinib is an epidermal growth factor receptor inhibitor (EGFR inhibitor). Erlotinib HCl was approved. Erlotinib binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. For the signal to be transmitted, two EGFR molecules need to come together to form a homodimer. These then use the molecule of ATP to trans-phosphorylate each other on tyrosine residues, which generates phosphotyrosine residues, recruiting the phosphotyrosine-binding proteins to EGFR to assemble protein complexes that transduce signal cascades to the nucleus or activate other cellular biochemical processes. When erlotinib binds to EGFR, formation of phosphotyrosine residues in EGFR is not possible and the signal cascades are not initiated.- Hamzehlou S, .et al. , Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Manabe A, .et al. , J Cell Physiol, 2018, Nov 21 PMID: 30461012
- Yui Takashina, .et al. , Nutrients, 2018, Oct; 10(10): 1345 PMID: 30241394
- Furukawa C, .et al. , J Cell Physiol, 2017, Oct;232(10):2841-2850 PMID: 27925186
- Xiaoyu Yang, .et al. , Free Radic Biol Med, 2016, Aug; 97: 342-350 PMID: 27368132
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IRAK-4 inhibitor
IRAK inhibitor 1 is a potent IRAK-4 inhibitor with IC50 of 216 nM, is poorly active against JNK-1 and JNK-2 with IC50 of 3.801 μM, and >10 μM, respectively. -
interleukin-1 receptor associated kinase inhibitor
IRAK inhibitor 2 is interleukin-1 receptor associated kinase inhibitor . -
IRAK modulator
IRAK inhibitor 3 is an interleukin-1 (IL-I) receptor-associated kinase (IRAK) kinase modulator extracted from patent WO2008030579 A2. -
IRAK4 inhibitor
IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4(IRAK4) inhibitor. -
IRAK inhibitor
IRAK-IN-6, also known as IRAK inhibitor 6, is an interleukin-1 receptor associated kinase 4 (IRAK-4) inhibitor. IRAK-4 is reported to be essential for the activation of the intracellular signalling cascades including NF-kB and MAPK pathways, which are critical for the production of inflammatory cytokines. - IRAK-1-4 inhibitor is a benzimidazole that disrupts the activity of IRAK-1 and -4 with IC50 values of 300 and 200 nM, respectively.
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Src inhibitor
KX2-391 2Hcl is 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. -
M-CSFR, CSF1R inhibitor
Ki 20227 is an inhibitor of c-Fms tyrosine kinase (M-CSFR, CSF1R).- Wensheng Wang, .et al. , J Bone Miner Res, 2017, May; 32(5): 939-950 PMID: 28052488
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VEGFR Inhibitor
Motesanib (AMG706) is a multikinase inhibitor that selectively targets VEGF receptors, platelet-derived growth factor receptors (PDGFRs), and Kit receptors with IC?? values of 2 nM (VEGFR1), 3 nM (VEGFR2), 6 nM (VEGFR3), 84 nM (PDGFR), and 8 nM (Kit).- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932