(+)-Enitociclib(Synonyms: (+)-BAY-1251152; (+)-VIP152)

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(+)-Enitociclib (Synonyms: (+)-BAY-1251152; (+)-VIP152) 纯度: 99.66%

(+)-Enitociclib ((+)-BAY-1251152) 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。

(+)-Enitociclib(Synonyms: (+)-BAY-1251152;  (+)-VIP152)

(+)-Enitociclib Chemical Structure

CAS No. : 1610358-56-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2029 In-stock
2 mg ¥1320 In-stock
5 mg ¥2280 In-stock
10 mg ¥3480 In-stock
50 mg ¥10680 In-stock
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200 mg   询价  

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(+)-Enitociclib 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

(+)-Enitociclib ((+)-BAY-1251152) is an enanthiomer of BAY-1251152 with rotation (+). (+)-Enitociclib is a potent and selective CDK9 inhibitor with an IC50 of 3 nM. (+)-Enitociclib has anti-tumour activity[1][2].

IC50 & Target[1]

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[1].
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’)[2].

上海金畔生物科技有限公司 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[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female SCID mice with OCI-LY-3 cells[2]
Dosage: 10 mg/kg
Administration: Intravenous injection; once every seven days; for 14 days
Result: Inhibited tumour growth and had good tolerability.

分子量

404.43

Formula

C19H18F2N4O2S

CAS 号

1610358-56-9

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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 113.3 mg/mL (280.15 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4726 mL 12.3631 mL 24.7262 mL
5 mM 0.4945 mL 2.4726 mL 4.9452 mL
10 mM 0.2473 mL 1.2363 mL 2.4726 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.18 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.18 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.18 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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