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Bcr-Abl Inhibitors (17)


Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1021 Dasatinib Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
  • Cell Stem Cell, 2012, 10(2):210-7
  • Cancer Discov, 2011, 1(7):608-25
  • J Exp Med, 2013, 210(11):2205-21
S1026 Imatinib Mesylate (STI571) Imatinib Mesylate (STI571) is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM, respectively.
  • Leukemia, 2014, 28(4):977-9
  • Leukemia, 2012, 27(4):932-40
  • Oncogene, 2014, 33(2):236-45
S1006 Saracatinib (AZD0530) Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Phase 2/3.
  • Nat Cell Biol, 2014, 16(5):401-14
  • Nat Cell Biol, 2013, 15(4):395-405
  • J Clin Invest, 2014, 124(12):5490-502
S1490 Ponatinib (AP24534) Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM, respectively.
  • Cancer Cell, 2012, 22(5):656-67
  • Sci Transl Med, 2014, 6(261):261ra152
  • Proc Natl Acad Sci U S A, 2014, 10.1073/pnas.1321173111
S1033 Nilotinib (AMN-107) Nilotinib (AMN-107) is a Bcr-Abl inhibitor with IC50 less than 30 nM.
  • Antimicrob Agents Chemother, 2014, 58(5):2598-607
  • FASEB J, 2011, 25(10):3661-73
  • Sci Rep, 2013, 3:2102
S7782 Dasatinib Monohydrate Dasatinib Monohydrate is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
S7269 PD173955 PD173955 is a potent Bcr-Abl inhibitor with IC50 of 1-2 nM, also inhibiting Src activity with IC50 of 22 nM.
S7526 GNF-5 GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM.
S1107 Danusertib (PHA-739358) Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2.
  • Cancer Res, 2014, 74(20):5878-90
  • Cancer Res, 2013, 73(20):6310-22
  • Biochem Pharmacol, 2012, 83(4):452-61
S1134 AT9283 AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM; also potent to Aurora A/B, Abl(T315I). Phase 2.
  • Cell Stem Cell, 2012, 11(2):179-94
  • Cancer Res, 2013, 73(20):6310-22
  • Cancer Lett, 2013, 341(2):224-30
S7194 GZD824 Dimesylate GZD824 Dimesylate 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.
S2158 KW-2449 KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR. Phase 1.
S2634 DCC-2036 (Rebastinib) DCC-2036 (Rebastinib) is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit. Phase 1.
  • Anal Chem, 2013, 85(15):6995-7002
  • PLoS One, 2013, 8(8): e73059
S2202 NVP-BHG712 NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.
  • Anticancer Res, 2014, 34(6):2913-8
S2899 GNF-2 GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl, shows no activity to Flt3-ITD, Tel-PDGFR, TPR-MET and Tel-JAK1 transformed tumor cells.
S1369 Bafetinib (INNO-406) Bafetinib (INNO-406) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit. Phase 2.
  • J Med Chem, 2015,
  • Int Arch Allergy Immunol, 2012, 159(1):15-22
S2243 Degrasyn (WP1130) Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT).
  • Trends Pharmacol Sci, 2014, 35(4):187-207
  • Oncogene, 2014, 10.1038/onc.2014.351
  • Neoplasia, 2012, 14(10):893-904

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