CAS number：937270-47-8 molecular formula：C23H24N4O
SB1317是一种强效的细胞周期蛋白依赖性激酶(CDKs)\FMS样酪氨酸激酶3(FLT3)及Janus激酶2(JAK2)抑制剂,对CDK2\JAK2及FLT3的IC50值分别为13 nM\56 nM及73 nM. CDKs是调节细胞周期的丝氨酸苏氨酸激酶.JAK2是一种不可逆的细胞内酪氨酸激酶,其经由JAK-STAT信号通路转导细胞因子介导的信号.FLT3是一种细胞因子受体,在造血干细胞的正常发展中发挥着重要作用. 在表达荧光素酶的MM1S细胞中,SB1317克服了IL-6赋予的增殖/保护优势.在MM1S细胞中,SB1317增加G2 / M期的细胞比例,且减少S期的细胞.另外,SB1317增加亚G0区的细胞数.在人多发性骨髓瘤浆细胞瘤异种移植CB17-SCID小鼠模型(硼替佐米敏感性MM1S模型和更具硼替佐米耐药性的OPM2模型)中,SB1317显著抑制肿瘤生长.在皮下AML模型中,连续21天每天给小鼠分别服用10\20或40 mg/kg剂量的SB1317可使平均肿瘤体积分别减小53%\61%及113%.
| Chinese alias | - | ||
| English alias | NSC762673 | NSC-762673 | EX-A7310 | 20-Oxa-5,7,14,27-tetraazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2,4,6(27),8,10,12(26),16,21,23-decaene, 14-methyl- | TG02 | 1204918-72-8 | AC-35951 | BS167349 | (E)-6-methyl-12-oxa-3,6-diaza-2(4,2)-pyrimidina-1,4( | ||
| CAS number | 937270-47-8 | molecular formula | C23H24N4O |
| molecular weight | 372.46 g/mol | Exact mass | - |
| PSA | 50.300 Ų | logp | 4.2 |
No numbering system information yet
No physical and chemical property information yet
No safety information yet
No production method and use information yet
No upstream information yet
No downstream information yet
