| Identification | Back Directory | [Name]
BMS-986260 | [CAS]
2001559-19-7 | [Synonyms]
BMS-986260
6-(4-(3-Chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidazol-5-yl)imidazo[1,2-b]pyridazine-3-carbonitrile
Imidazo[1,2-b]pyridazine-3-carbonitrile, 6-[4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidazol-5-yl]-
nuclear translocation,TGFβR1,BMS-986260,FOXP3 expression,MINK,Transforming growth factor beta receptors,oral,NHLF cells,BMS986260,inhibit,Inhibitor,CD25,TGF-β Receptor,pSMAD2/3,selective,BMS 986260 | [Molecular Formula]
C18H12ClFN6O | [MDL Number]
MFCD34471674 | [MOL File]
2001559-19-7.mol | [Molecular Weight]
382.78 |
| Chemical Properties | Back Directory | [density ]
1.52±0.1 g/cm3(Predicted) | [solubility ]
DMSO: Sparingly soluble: 1-10 mg/ml
Ethanol: Slightly soluble: 0.1-1 mg/ml | [form ]
Solid | [pka]
14.46±0.10(Predicted) | [color ]
Light yellow to brown |
| Hazard Information | Back Directory | [Uses]
BMS-986260, an immuno-oncology agent, is a potent, selective, and orally active TGFβR1 inhibitor (IC50=1.6 nM). BMS-986260 displays exquisite selectivity for TGFβR1 over its isozyme TGFβR2, as well as in a panel of more than 200 kinases examined. BMS-986260 inhibits TGFβ mediated nuclear translocation of pSMAD2/3 in MINK and NHLF cells lines with an IC50 of 350 nM and 190 nM, respectively[1]. | [References]
[1] Velaparthi U, et al. Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent. ACS Med Chem Lett. 2020;11(2):172-178. Published 2020 Jan 28. DOI:10.1021/acsmedchemlett.9b00552 |
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