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Catalog No.
Product Name
Application
Product Information
Product Citation
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VEGFR/PDGFRβ/KIT inhibitor
N-desethyl sunitinib is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor (Ki values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT respectively). -
Bcr-Abl inhibitor
Nilotinib is a Bcr-Abl inhibitor with IC50 less than 30 nM. -
FGFR Inhibitor
NVP-BGJ398 phosphate is a novel selective, pan-specific FGFR inhibitor with IC50 of 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively; >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. -
Tyrosine kinase inhibitor
Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. -
VEGFR Inhibitor
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). -
VEGFR2/Src kinase inhibitor
TG 100572 is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nM for VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively. -
VEGFr2 inhibitor
TG 100801 is the prodrug of TG 100572 (HY-10184), TG 100572 is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nM or VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively. -
c-Kit/VEGFR2/PDGFRβ inhibitor
Toceranib phosphate is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ. -
VEGFR inhibitor
Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM. -
VEGFR/EGFR inhibitor
Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM. -
CSF1/Kit/FLT3 inhibitor
Pexidartinib is a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity.- Lu Luo, .et al. , J Neuroinflammation, 2022, Jun 11;19(1):141 PMID: 35690810
- Sarah R Anderson,, .et al. , bioRxiv, 2022, 01.05.475126
- Hannah D Mason, .et al. , JCI Insight, 2021, Oct 8;6(19):e149229 PMID: 34428178
- Chritica Lodder, .et al. , Acta Neuropathol Commun, 2021, Jun 8;9(1):108 PMID: 34103079
- Anderson SR, .et al. , Cell Rep, 2019, May 14;27(7):2002-2013.e5 PMID: 31091440
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Syk inhibitor
PRT-060318 is a novel selective inhibitor of the tyrosine kinase Syk, as an approach to HIT treatment. -
EGFR inhibitor
AZD3759 is an orally available inhibitor of the epidermal growth factor receptor (EGFR). It binds to and inhibits the activity of EGFR as well as certain mutant forms of EGFR. -
BTK inhibitor
ONO-4059 is a highly potent and selective oral BTK inhibitor -
FAK inhibitor
GSK2256098 is a focal adhesion kinase-1 (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. -
MET/VEGFR-2 inhibitor
BMS-817378 is a novel prodrug of the dual Met/VEGFR-2 inhibitor BMS-794833. -
HIF-PHD Inhibitor II
JNJ-42041935 is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes. -
TRK, ROS1, ALK inhibitor
Entrectinib, also known as RXDX-101 and NMS-E628, is an oral small molecule inhibitor of TrkA, TrkB and TrkC, as well as ROS1 and ALK, with high potency and selectivity. -
Btk Inhibitor
ACP-196 is an orally available inhibitor of Bruton?€?s tyrosine kinase (BTK) with potential antineoplastic activity. It inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. -
Irreversible FGFR inhibitor
FIIN-3 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor. -
Bcr-Abl Inhibitor
GZD824 is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively. -
EGFR Inhibitor
AG-18 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 35 ,M in the human epidermoid carcinoma cell line A431. -
FGFR2 Inhibitor
Alofanib is a potent and selective allosteric inhibitor of FGFR2 with potential anticancer activity. -
FGFR inhibitor
Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. -
BTK inhibitor
Olmutinib is a potent small molecule inhibitor of Bruton's tyrosine kinase (BTK). -
ALK2 inhibitor
LDN-214117 is a selective and potent ALK2 inhibitor. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM. -
HIF-2a translation inhibitor
HIF-2a translation inhibitor (IC50 value 5 uM); Decreases HIF-2a protein and HIF-2a target gene expression in normoxia and hypoxia independent of HIF-2a mRNA expression or HIF-2a protein stability, and independent of mTOR activity. Moreover, the translation inhibitor 76 enhances binding of IRP1 to the HIF-2a IRE (Iron-Responsive Element). -
RTK inhibitor
Nintedanib is a potent inhibitor of multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs).- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
- Thibaut Fourniols, .et al. , Int J Pharm, 2020, Jun 30;584:119337 PMID: 32371002
