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Catalog No.
Product Name
Application
Product Information
Product Citation
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EGFR inhibitor
AST-6 is a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, inhibits tumor growth both in vitro and in vivo -
c-Met inhibitor
BMS-794833 is a potent ATP competitive inhibitor to Met and VEGFR-2 with IC50 of 1.7 and 15 nmol. -
c-Met inhibitor
MGCD265 is a multitargeted tyrosine kinase inhibitor that binds to and inhibits the phosphorylation of several RTKs, including the c-Met receptor (HGFR); the Tek/Tie-2 receptor; VEGFR types 1, 2, and 3; and MST1R. -
EGFR Inhibitor
OSI-420 (Desmethyl Erlotinib,CP-473420) is an orally active EGFR tyrosin kinase inhibitor, which inhibits receptor tyrosine kinases (TKs) by inhibition of the intercellular domain .- Yuta Yamamoto, .et al. , J Pharm Anal, 2018, Apr; 8(2): 119-123 PMID: 29736298
- Janet L. Martin, .et al. , Breast Cancer Res, 2017, 19: 90 PMID: 28778177
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Aurora inhibitor
Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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Syk Inhibitor
R406 is an orally available spleen tyrosine kinase inhibitor with an IC50 of 41 nM. -
RAF/VEGFR Inhibitor
Raf265 derivative is a derivative of Raf265 that is an oral, highly selective RAF and VEGFR kinase inhibitor with IC50 of of 5 to 10 μM. -
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. -
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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FAK inhibitor
PF-562271 is an orally bioavailable small molecule and ATP-competitive focal adhesion kinase (FAK) inhibitor with potential antineoplastic and antiangiogenic activities.- Jiping Yue, .et al. , Nat Commun, 2016, 7: 11692 PMID: 27216888
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Syk Inhibitor
BAY 61-3606 is a cell-permeable imidazopyrimidine compound that acts as a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity with no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src.- So-Jeong Park, .et al. , Ecotoxicol Environ Saf, 2023, Jul 15;260:115061 PMID: 37257343
- Ami Kobayashi, .et al. , Nat Commun, 2023, Jan 25;14(1):312 PMID: 36697396
- Ju-Won Jang, .et al. , Int Immunopharmacol, 2021, Mar 21;95:107509 PMID: 33761438
- Sojin Park, .et al. , Sci Rep, 2020, 10: 11784 PMID: 32678160
- Park S, .et al. , Free Radic Res, 2018, Sep 11:1-11 PMID: 30203714
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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. -
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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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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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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FAK inhibitor
NVP-TAE226 is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2(IC50=3.5 nM); 10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met.- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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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. -
Syk inhibitor
P505-15 (also known as PRT062607) is a novel, highly selective, and orally bioavailable small molecule SYK inhibitor (SYK IC(50) = 1 nM) with anti-SYK activity that is at least 80-fold greater than its affinity for other kinases.- Li T, .et al. , Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
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Raf kinase inhibitor
Sorafenib N-Oxide is a metabolite of Sorafenib, a potent Raf kinase inhibitor. - (-)-Catechin gallate is an antioxidant constituent of green tea. At uM concentrations, inhibits VEGF-induced tyrosine phosphorylation.
- MS Islam ,etc. Effect of UV Irradiation on the Nutritional Quality and Cytotoxicity of Apple Juice. Journal of Agricultural and Food Chemistry, 2016, 64(41), 7812-7822.
- MS Islam ,etc. UV-C irradiation as an alternative disinfection technique: Study of its effect on polyphenols and antioxidant activity of apple juice. Innovative Food Science & Emerging Technologies, 2016, 34, 344-351.
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multi-targeted tyrosine kinase inhibitor
Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor with IC50s of 4, 20, 4, 2 nM for KDR, Flt-1, FGFR1 and PDGFRα, respectively. -
BTK inhibitor
GDC-0834 Racemate is a potent and selective inhibitor of Bruton's tyrosine kinase (BTK), investigated as a potential treatment for rheumatoid arthritis. -
SYK inhibitor
Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. -
Bcr-Abl tyrosine inhibitor?€?
Radotinib is a novel and selective Bcl-Abl tyrosine kinase inhibitor -
Bcr-Abl inhibitor
PD-173955 is a src tyrosine kinase inhibitor. PD173955 inhibited Bcr-Abl-dependent cell growth. PD173955 showed cell cycle arrest in G(1). PD173955 has an IC(50) of 1-2 nM in kinase inhibition assays of Bcr-Abl, and in cellular growth assays it inhibits Bcr-Abl-dependent substrate tyrosine phosphorylation. PD173955 inhibited kit ligand-dependent c-kit autophosphorylation (IC(50) = approximately 25 nM) and kit ligand-dependent proliferation of M07e cells (IC(50) = 40 nM) but had a lesser effect on interleukin 3-dependent (IC(50) = 250 nM) or granulocyte macrophage colony-stimulating factor (IC(50) = 1 microM)-dependent cell growth. -
EGFR inhibitor
CL-387785 is an irreversible inhibitor of EGFR with IC50 of 370+/-120 pM; is able to overcome resistance caused by the T790M mutation on a functional level. -
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. -
c-Abl/c-Kit/PDGRFβ inhibitor
Flumatinib mesylate can reduce the expression of C-MYC, HIF-1 a and VEGF in U266 cell line in a time- and dose-dependent manners, so flumatinib mesylate may become a new drug for MM therapy. -
EGFR Inhibitor
EGFR inhibitor is a cell permeable, 4,6-disubstituted pyrimidine compound that selectively inhibits the EGFR kinase with an IC50 value of 21 nM in vitro and blocks receptor autophosphorylation in cells. -
EGFR inhibitor
CNX-2006 is a potent, mutant-selective EGFR inhibitor with excellent in vitro activity in cells with activating EGFR mutations, as well as in cells harbouring the T790M mutation. CNX-2006 is the prototype for CO-1686, which is currently in a Phase I clinical trial for the treatment of EGFR-mutant lung cancer. -
HIF-PH inhibitor
DMOG is a cell permeable, competitive inhibitor of HIF-PH. It acts to stabilize HIF-1α expression at normal oxygen tensions in cultured cells, at concentrations between 0.1 and 1 mM.- Hideaki Nakamura, .et al. , PLoS One, 2018, 13(2): e0192136 PMID: 29466367
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Dual Syk and JAK inhibitor
PRT062070 is a novel, oral, dual spleen tyrosine kinase (Syk) and janus kinase (JAK) inhibitor. Cerdulatinib preferentially inhibited JAK1 and JAK3 dependent cytokine mediated signaling and functional responses in various cell types. - Oroxylin A is an O-methylated flavone, It has demonstrated activity as a dopamine reuptake inhibitor and is also a negative allosteric modulator of the benzodiazepine site of the GABAA receptor.
- Paramesha Bugga, .et al. , Cell Signal, 2022, Jun;94:110309 PMID: 35304284
- Bugga Paramesha, .et al. , Antioxidants (Basel), 2021, Feb 24;10(3):338 PMID: 33668369
- Mai Nagasaka, .et al. , Molecules, 2018, Jun; 23(6): 1394 PMID: 29890668
