Enitociclib

(Synonyms: (+)-Enitociclib; (+)-BAY-1251152; (+)-VIP152; (S)-Enitociclib)
目录号: PL01373 纯度: ≥99%
Enitociclib ((+)-Enitociclib) 是 BAY-1251152 的一个对映体,旋光性为 (+)。Enitociclib 是一种有效的选择性 CDK9 抑制剂,IC50 为 3 nM。Enitociclib 具有抗肿瘤活性。
CAS No. :1610358-56-9
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中文名称
Enitociclib
英文名称
Enitociclib
英文别名
5-fluoro-4-(4-fluoro-2-methoxyphenyl)-N-[4-[(methylsulfonimidoyl)methyl]pyridin-2-yl]pyridin-2-amine;(+)-5-Fluoro-4-(4-fluoro-2-methoxyphenyl)-N-[4-[(S-methylsulfonimidoyl)methyl]pyridin-2-yl]pyridin-2-amine;BCP29512;BCP33292;NSC802450;BAY1251152;(Inverted exclamation markA)-BAY-1251152;(+)-BAY-1251152;Enitociclib
Cas No.
1610358-56-9
分子式
C19H18F2N4O2S
分子量
404.43
包装储存
Powder -20°C 3 years;4°C 2 years
详情描述
Enitociclib ((+)-Enitociclib) 是 BAY-1251152 的一个对映体,旋光性为 (+)。Enitociclib 是一种有效的选择性 CDK9 抑制剂,IC50 为 3 nM。Enitociclib 具有抗肿瘤活性。
产品详情
Enitociclib ((+)-Enitociclib) 是 BAY-1251152 的一个对映体,旋光性为 (+)。Enitociclib 是一种有效的选择性 CDK9 抑制剂,IC50 为 3 nM。Enitociclib 具有抗肿瘤活性。
生物活性
Enitociclib ((+)-Enitociclib) is an enanthiomer of BAY-1251152 with rotation (+). Enitociclib is a potent and selective CDK9 inhibitor with an IC 50 of 3 nM. Enitociclib has anti-tumour activity.
性状
Solid
IC50 & Target[1][2]
CDK9/CycT1 3 nM (IC50)
体外研究(In Vitro)
Enitociclib (Example 2) inhibits HeLa, HeLa-MaTu-ADR, NCI-H460, DU145, Caco-2, B16F10, A2780 and MOLM-13 cells proliferation with IC50 values of 110 nM, 33 nM, 75 nM, 33 nM, 62 nM, 240 nM, 110 nM and 29 nM, respectively.
An efficient inhibition of the proliferation of both ABC (Activated B-cell type) and GCB (Germinal-centre B-cell type) subtypes of diffuse large B-cell lymphoma (DLBCL) by Enitociclib (Compound A). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Enitociclib (Compound A’; 10 mg/kg; intravenous injection; once every seven days; for 14 days; female SCID mice) treatment reaches a Treatment to Control ratios (T/C) by area of 0.29 and a T/C by weight of 0.24. Enitociclib inhibits tumour growth and had good tolerability. 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]. Ulrich LüCKING, et al. 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfoximine group. WO2014076091A1.
[2]. Use of Arne Scholz, et al. 5-fluoro-4-(4-fluoro-2-methoxyphenyl)-n-{4-[(s-methylsulfonimidoyl)methyl]pyridin-2-yl}pyridin-2-amine for treating diffuse large b-cell lymphoma. WO2019158517A1.
溶解度数据
In Vitro: DMSO : 113.3 mg/mL (280.15 mM; Need ultrasonic and warming)配制储备液
搜索质检报告(COA)
[1]. Ulrich LüCKING, et al. 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfoximine group. WO2014076091A1.
[2]. Use of Arne Scholz, et al. 5-fluoro-4-(4-fluoro-2-methoxyphenyl)-n-{4-[(s-methylsulfonimidoyl)methyl]pyridin-2-yl}pyridin-2-amine for treating diffuse large b-cell lymphoma. WO2019158517A1.

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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