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Aurora A/B Kinase inhibitor
PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1. -
Src inhibitor
KX2-391 is a novel non-ATP competitive substrate-pocket directed SRC inhibitor.
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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. -
EGFR inhibitor
BIBX 1382 is a cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR. -
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. -
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. -
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. -
VEGFR1/2/3/PDGFRβ/Kit/RET/Raf-1 inhibitor
Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively. -
multi-targeted receptor tyrosine kinases inhibitor
SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT. -
VEGFR Antagonist
Buflomedil is a vasoactive agent used to treat peripheral vascular disease. -
ALK inhibitor
ALK-IN-1, an analog of AP26113, is an orally-available, potent, and selective inhibitor of ALK with a potency of 0.62 nM against wild-type and activity against a wide range of mutants, including the crizotinib-resistant L1196M line.
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EGFR inhibitor
AG-17 is an inhibitor of EGF receptor kinase with an IC50 value of 460 μM in the human epidermoid carcinoma cell line A431. -
VEGFR Inhibitor
ZM 323881 is a potent and selective inhibitor of the kinase activity of the human vascular endothelial growth factor receptor 2 (VEGFR2/KDR). -
FLT3 inhibitor
TG-02 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor. - (-)-Gallocatechin possesses free radical scavenging ability. It inhibits the growth and adherence of P. gingivalis onto the buccal epithelial cells.
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Raf kinase inhibitor
Sorafenib N-Oxide is a metabolite of Sorafenib, a potent Raf kinase inhibitor. -
Thalidomide-based Cereblon ligand
Thalidomide fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.
- Picropodophyllin (AXL1717) is the first targeted oral small-molecule IGF-1 receptor inhibitor with no effect on the insulin receptor.
- Scutellarin, a main active ingredient extracted from Erigeron breviscapus (Vant.) Hand-Mazz, has been wildly used to treat acute cerebral infarction and paralysis induced by cerebrovascular diseases.
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CDK/JAK2/FLT3 inhibitor
SB1317 is a potent inhibitor of Cyclin dependent kinases (CDKs), FMS-like tyrosine kinase-3 (FLT3) and Janus kinase 2 (JAK2) with IC50 values of 13nM, 56nM and 73nM for CDK2, JAK2 and FLT3, respectively. -
Tie-2 inhibitor
AMG-Tie2-1 is a highly potent, non-selective inhibitor of Tie-2 (IC50 <1 nM).

