Catalog No.
Product Name
Application
Product Information
Product Citation
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IGF-1R inhibitor
NVP-ADW742 is an IGF-1R inhibitor with IC50 of 0.17 μM.- Kazuya Takayama, .et al. , Sci Rep, 2018, 8: 8278 PMID: 29844341
- Kentaro Hirose, .et al. , BMC Dev Biol, 2014, 14: 42. PMID: 25480380
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EphB4 inhibitor
NVP-BHG712 is a selective inhibitor of EphB4 kinase that exhibits selectivity for EphB4 over more than 40 other kinases in vitro, including FGFR3.- Y Kaibori, .et al. , the FASEB Journal, 2019, Jan 22:fj201801519RR PMID: 30668924
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ALK Inhibitor
TAE684 is a inhibitor of ALK and also a potent inhibitor of LRRK2 kinase activity (IC(50) of 7.8nM against wild-type LRRK2, 6.1nM against the G2019S mutant).- Yue Guo, .et al. , Cell Biosci, 2022, Dec 30;12(1):210 PMID: 36585695
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Li T, .et al. , Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
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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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VEGFR/PDGFR/FGFR inhibitor
Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Hideharu Yamada, .et al. , Oncol Lett, 2021, Jun;21(6):455 PMID: 33907565
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
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EGFR inhibitor
PD153035 is an extremely potent and specific inhibitor of the tyrosine kinase activity of EGFR. -
FGFR1/VEGFR2 Inhibitor
PD173074 is a potent, cell permeable and ATP competitive inhibitor of FGFR and VEGFR.- Cheryl Q.E. Lee, .et al. , Stem Cell Reports, 2016, Feb 9; 6(2): 257-272 PMID: 26862703
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EGFR inhibitor
Pelitinib (EKB-569) is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity.- Shi P, .et al. , Transl Oncol, 2019, Mar 8;12(5):705-713 PMID: 30856555
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c-Met Inhibitor
PF-04217903 is a novel c-Met/hepatocyte growth factor receptor tyrosine kinase inhibitors. -
ALK/ c-Met inhibitor
PF-2341066 (Crizotinib) is an inhibitor of the c-Met kinase and the NPM-ALK. PF-2341066 inhibited cell proliferation in ALK-positive ALCL cells (IC50s=30 nM).- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Yu B, .et al. , J Sep Sci, 2020, Jan 22 PMID: 31970927
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Li T, .et al. , Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
- Saki Omote, .et al. , Sci Rep, 2018, 8: 9237 PMID: 29915248
- Arakawa H, .et al. , J Pharm Sci, 2017, Sep;106(9):2899-2903 PMID: 28336299
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c-Met Inhibitor
PHA665752 is a small-molecule inhibitor of c-Met/HGF/SF signaling. -
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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MAO-B inhibitor
Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C. -
Syk Inhibitor
R406 is an orally available spleen tyrosine kinase inhibitor with an IC50 of 41 nM.- Gabriella Leung, .et al. , JCI insight, 2021, Dec 8;6(23):e149376 PMID: 34673575
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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 (CHIR-265) is an oral, highly selective RAF and VEGFR kinase inhibitor, which is to control or normalize VEGFR-2 along with the inhibition of B-raf and c-Raf mutation to prevent cancers. -
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. -
RTK inhibitor
Sunitinib is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST).- Chern Ein Oon, .et al. , World J Gastrointest Oncol, 2023, May 15;15(5):810-827 PMID: 37275453
- Rachel K Toth, .et al. , Cells, 2022, Mar 16;11(6):1006 PMID: 35326457
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Thibaut Fourniols, .et al. , Int J Pharm, 2020, Jun 30;584:119337 PMID: 32371002
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
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FLT3 Inhibitor
Tandutinib (MLN518) inhibits the autophosphorylation of FLT3, c-KIT and PDGF receptor tyrosine kinases, thereby inhibiting cellular proliferation and inducing apoptosis. -
VEGFR-2 Inhibitor
Taxifolin is found to bind at the ATP-binding site on VEGFR-2 kinase with large value of binding energy and act as type I competitive inhibitor.- Keji Yu, .et al. , Nat Commun, 2022, Jun 14;13(1):3425 PMID: 35701431
- Shinji Kondo, .et al. , Curr Issues Mol Biol, 2021, Sep 26;43(3):1293-1306 PMID: 34698101
- Shin-ichi Adachi, .et al. , Cytotechnology, 2017, Apr; 69(2): 329-336 PMID: 28101741
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p38 MAPK inhibitor
Pexmetinib is a potent inhibitor of cytokine synthesis, via the dual inhibition of p38 mitogen-activated protein kinase (MAPK), and Tie2/Tek receptor tyrosine kinase. -
VEGFR-2 inhibitor
Telatinib (BAY 57-9352) is an orally available, small-molecule inhibitor of vascular endothelial growth factor receptors 2 and 3 (VEGFR-2/-3) and platelet-derived growth factor receptor β tyrosine kinases. -
Tie2 kinase inhibitor
Tie2 kinase inhibitor is a potent and selective Tie2 inhibitor with IC50 of 0.25 μM. -
PDFGRβ inhibitor
Orantinib (TSU-68, SU6668) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3.- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
- Aaron Y. Lai, .et al. , Brain, 2015, Apr;138(Pt 4):1046-58 PMID: 25688079
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VEGFR inhibitor
Vandetanib (Zactima) is a VEGFR and EGFR antagonist and a tyrosine kinase inhibitor with IC50 of 60, 90, 40 nM for HUVEC proliferation, PC-9 cells and tyrosine kinase activity, respectively.- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Shinya Kitamura, .et al. , Biochem Biophys Res Commun, 2020, Aug 13 PMID: 32800552
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
- Rintaro Sogawa, .et al. , JPA, 2018, in Press PMID: 30740257
- Park K, .et al. , Anat Sci Int, 2018, Jun;93(3):372-383 PMID: 29256114
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Park K, .et al. , Biomed Pharmacother, 2016, Mar;78:140-149 PMID: 26898435
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VEGFR inhibitor
Vatalanib (PTK787 or PTK/ZK) is a small molecule protein kinase inhibitor that inhibits angiogenesis that inhibits all known VEGF receptors, as well as platelet-derived growth factor receptor-beta and c-kit, but is most selective for VEGFR-2. CAS: 212141-51-0 (HCl) 212141-54-3 (Free base)- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
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VEGFR inhibitor
XL184 free base (Cabozantinib) is a small molecule designed to inhibit multiple receptor tyrosine kinases, specifically MET and VEGFR2.- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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c-MET inhibitor
Foretinib (GSK1363089), a multikinase inhibitor of c-Met and VEGFR-2, blocks proliferation, induces Anoikis, and impairs ovarian cancer metastasis.- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
- Narges K Gortany, .et al. , Cancer Chemother Pharmacol, 2021, Mar 10 PMID: 33688998
- Hamzehlou S, .et al. , Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Hayato Ogura, .et al. , Sci Rep, 2017, 7: 5519 PMID: 28717217
- Fuse MJ, .et al. , Mol Cancer Ther, 2017, Oct;16(10):2130-2143 PMID: 28751539
- Ryohei Katayama, .et al. , Clin Cancer Res, 2015, Jan 1; 21(1): 166-174 PMID: 25351743
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IGF-1R inhibitor
NVP-AEW541 is a selective IGF-1R kinase inhibitor that inhibits the autophosphorylation activity of IGF-1R (IC50 = 0.086 uM) and prevents IGF-1-mediated survival and proliferation of MCF-7 cells (IC50 = 0.16 and 1.64 uM, respectively).- Deep R Sharma, .et al. , Cereb Cortex, 2023, Jan 16 PMID: 36646459
- Ashalyn P Watt, .et al. , Cell Tissue Res, 2021, Jan 13 PMID: 33439347
- Tsushima H, .et al. , Autoimmunity, 2017, Aug;50(5):329-335 PMID: 28682648
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EGFR Inhibitor
AG-1478 (Tyrphostin AG-1478) is an inhibitor of EGFR kinase with an IC50 value of 3 nM.- Khattab M, .et al. , J Phys Chem B, 2018, May 3;122(17):4667-4679 PMID: 29629773
- Muhammad Khattab, .et al. , Sci Rep, 2017, 7: 16271 PMID: 29176733
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HER2 Inhibitor
ARRY-380 is an ErbB-2 inhibitor that selectively binds to and inhibits the phosphorylation of ErbB-2, resulting in growth inhibition and death of ErbB-2-expressing tumor cells. -
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