For research use only. Not for therapeutic Use.
DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo[1].
DS-1205b (0.3-33 μM; 2-24 h) inhibits hGAS6-induced migration in NIH3T3-AXL cells (EC50=2.7 nM)[1].
DS-1205b (1-10000 μM; 2-24 h) significantly inhibits the phosphorylation of AXL in NIH3T3-AXL cells. DS-1205b decreases NIH3T3 cell proliferation but not obviously inhibits growth (GI50>10,000 nM)[1].
DS-1205b (3.1-50 mg/kg; p.o. bid for 5 d) exhibits pAXL inhibition mediated antitumor effects in mice[1].
| Catalog Number | I026539 |
| CAS Number | 1855860-24-0 |
| Synonyms | N-[4-[2-amino-5-[4-[[(2R)-1,4-dioxan-2-yl]methoxy]-3-methoxyphenyl]pyridin-3-yl]-3-fluorophenyl]-5-(5-methylpyridin-2-yl)-1-(oxan-4-ylmethyl)-4-oxopyridine-3-carboxamide |
| Molecular Formula | C41H42FN5O7 |
| Purity | ≥95% |
| InChI | InChI=1S/C41H42FN5O7/c1-25-3-7-36(44-18-25)33-21-47(20-26-9-11-51-12-10-26)22-34(39(33)48)41(49)46-29-5-6-31(35(42)17-29)32-15-28(19-45-40(32)43)27-4-8-37(38(16-27)50-2)54-24-30-23-52-13-14-53-30/h3-8,15-19,21-22,26,30H,9-14,20,23-24H2,1-2H3,(H2,43,45)(H,46,49)/t30-/m1/s1 |
| InChIKey | ZOEILZXFYPPMTR-SSEXGKCCSA-N |
| SMILES | CC1=CN=C(C=C1)C2=CN(C=C(C2=O)C(=O)NC3=CC(=C(C=C3)C4=C(N=CC(=C4)C5=CC(=C(C=C5)OCC6COCCO6)OC)N)F)CC7CCOCC7 |
| Reference | [1]. Jimbo T, et, al. DS-1205b, a novel selective inhibitor of AXL kinase, blocks resistance to EGFR-tyrosine kinase inhibitors in a non-small cell lung cancer xenograft model. Oncotarget. 2019 Aug 27;10(50):5152-5167. |
