BMS-265246
目录号: PL12258 纯度: ≥99%
CAS No. :582315-72-8
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中文名称
BMS-265246
中文别名
(4-丁氧基-1H-吡唑并(3,4-b)吡啶-5-基)(2,6-二氟-4-甲基苯基)-甲酮;(4-丁氧基-1H-吡唑并[3,4-B]吡啶-5-基)(2,6-二氟-4-甲基苯基)-甲酮;BMS265246 抑制剂
英文名称
BMS-265246
英文别名
BMS-265246;(4-butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)-(2,6-difluoro-4-methylphenyl)methanone;(4-butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)(2,6-difluoro-4-methylphenyl)methanone;BMS265246;BMS-265246 (BMS265246);BMS-269233;BMS 265246;MLS006011031;BDBM5776;AOB6859;C18H17F2N3O2;HMS3655J09;BCP02546;2276AH;s2014;SB19464;BCP9000425;AK241904;SMR004702826;SW
Cas No.
582315-72-8
分子式
C18H17F2N3O2
分子量
345.34
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
BMS-265246 是一种有效且选择性的周期蛋白依赖性激酶 CDK1 和 CDK2 抑制剂,IC50 分别为 6 nM 和 9 nM。BMS-265246 可抑制 CHI3L1 刺激 ACE2 (血管紧张素转换酶 2) 和 SPP (病毒刺尖蛋白启动蛋白酶)。BMS-265246 可用于卵巢癌和 COVID-19 研究。
生物活性
BMS-265246 is a potent and selective cyclin-dependent kinase CDK1 and CDK2 inhibitor, with IC 50 values of 6 and 9 nM, respectively. BMS-265246 inhibits CHI3L1 (chitinase 3-like-1) stimulation of ACE2 (angiotensin converting enzyme 2) and SPP (viral spike protein priming proteases). BMS-265246 can be used for ovarian cancer and COVID-19 research.
性状
Solid
IC50 & Target[1][2]
CDK1/cycB 6 nM (IC50) CDK2/Cyc E 9 nM (IC
体外研究(In Vitro)
BMS-265246 binds at the ATP site and shows cytotoxic activity in ovarian cancer cell (A2780), with an IC50 of 0.76 μM.
BMS-265246 (0-10 μM) can dose dependently increase iTreg cell differentiation.
BMS-265246 (9 nM, 24 h) inhibits the ability of CHI3L1 to stimulate epithelial cells ACE2 and SPP.
BMS-265246 (1 μM, 1 h) prevents E2 induction of EGF3, AREG and CXCL12 in MCF7 cells.
BMS-265246 is able to cooperate with Tamoxifen to induce apoptosis in MCF7 cells. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Misra RN, Xiao H, Rawlins DB et al. 1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2405-8.
[2]. Gu H, et al. Inhibition of CDK2 promotes inducible regulatory T-cell differentiation through TGFβ-Smad3 signaling pathway. Cell Immunol. 2014 Jul;290(1):138-44.
溶解度数据
In Vitro: DMSO : 12.5 mg/mL (36.20 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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