| CAS NO. |
Products Name |
| 1952251-28-3 |
TAK659 |
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| TAK-659 hydrochloride is a potent, selective and orally available spleen tyrosine kinase (Syk) inhibitor with an IC50 of 3.2 nM. |
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| 1707289-21-1 |
BLU554 |
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| Fisogatinib (BLU-554) is a potent, highly selective and orally active fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 5 nM. Fisogatinib has significant anti-tumor activity in models of hepatocellular carcinoma (HCC) that are dependent on FGFR4 signalling |
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| 648903-57-5 |
BAY61-3606 2hcl |
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| BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM[1]. BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell[2]. BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates[3]. Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells |
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| 1702259-66-2 |
H3B-6527 |
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| H3B-6527 (H3 Biomedicine) is a highly selective FGFR4 inhibitor with potent antitumour activity in FGF19 amplified cell lines and mice. |
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| 1174161-86-4 |
SCR-1481B1 |
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| SCR-1481B1 (c-Met inhibitor 2) is a potent compound that has activity against cancers dependent upon Met activation and also has activity against cancers as a VEGFR inhibitor. |
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| 330786-25-9 |
PCI29732 |
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| PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay. IC50 value: 8.2 nM [1] Target: Btk kinase PCI 29732(compound 1) has a 8.2 nM potency against Btk in a FRET based biochemical enzymology assay. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase, probably due to the difference at the “gatekeeper” residue [1]. In human CD20+ B cells stimulated at the BCR, PCI-29732 blocked the transcriptional up-regulation of a panel of B-cell activation genes that occurs within 6 h of stimulation. Pulse exposure to the reversible inhibitor PCI-29732 did not result in BCR inhibition |
|
| 1402709-93-6 |
CCT241736 |
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| CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM; Aurora-B Kd, 48 nM), FLT3 kinase (Kd, 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd, 38 nM) and FLT3(D835Y) (Kd, 14 nM). |
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| 1448169-71-8 |
TAS120(Futibatinib) |
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| Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor. Futibatinib (TAS-120) covalently binds to a highly conserved P-loop cysteine residue in the ATP pocket of FGFR. Futibatinib (TAS-120) exhibits potency at low nanomolar concentrations and high specificity against wild-type FGFR1/2/3/4 as well as against some FGFR2 kinase domain mutations |
|
| 1234356-69-4 |
Derazantinib |
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| Derazantinib (ARQ-087) is an ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC50s of 4.5, 1.8, and 4.5 nM, respectively. |
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| 1313725-88-0 |
Savolitinib |
more... |
| Savolitinib (AZD-6094) is a potent, highly selective, and orally bioavailable c-Met inhibitor with IC50 s of 5 nM and 3 nM for c-Met and p-Met, respectively. Savolitinib (AZD-6094) selectively binds to and inhibits the activation of c-Met in an ATP-competitive manner, and disrupts c-Met signal transduction pathways. Antineoplastic activity |
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