中文名 | BMS-986260 |
英文名 | BMS-986260 |
别名 | 化合物BMS986260 6-(4-(3-氯-4-氟苯基)-1-(2-羟基乙基)-1H-咪唑-5-基)咪唑并[1,2-B]哒嗪-3-甲腈 |
英文别名 | BMS986260 BMS-986260 6-(4-(3-Chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidazol-5-yl)imidazo[1,2-b]pyridazine-3-carbonitrile |
CAS | 2001559-19-7 |
化学式 | C18H12ClFN6O |
分子量 | 382.78 |
溶解度 | 溶于DMSO |
存储条件 | -20℃ |
产品用途 | BMS-986260 is a potent, selective, and orally bioavailable TGFβR1 inhibitor (IC50=1.6 nM). BMS-986260 demonstrated functional activity in multiple TGFβ- dependent cellular assays, excellent kinome selectivity, favorable pharmacokinetic properties, and curative in vivo efficacy in combination with anti-PD-1 antibody in murine colorectal cancer (CRC) models。 |
参考资料 展开查看 | Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology AgentUpender Velaparthi*Chetan Padmakar DarneJayakumar WarrierPeiying LiuHasibur RahamanKaren Augustine-RauchKaren ParrishZheng YangJesse SwansonJennifer BrownGopal DharAravind AnandamVinay K. HolenarsipurKamalavenkatesh PalanisamyBarri S. WautletMark P. FereshtehJonathan LippyAndrew J. TebbenSteven SheriffMax RuzanovChunhong YanAnuradha GuptaArun Kumar GuptaMuthalagu VetrichelvanArvind MathurMarina GelmanRajinder SinghTodd KinsellaAnwar MurtazaJoseph FargnoliGregory ViteRobert M. BorzilleriACS Medicinal Chemistry Letters, Articles ASAP (Letter)Subscribed AccessPublication Date (Web):January 28, 2020。 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.612 ml | 13.062 ml | 26.124 ml |
5 mM | 0.522 ml | 2.612 ml | 5.225 ml |
10 mM | 0.261 ml | 1.306 ml | 2.612 ml |
5 mM | 0.052 ml | 0.261 ml | 0.522 ml |
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