Mevociclib(Synonyms: SY-1365)

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Mevociclib (Synonyms: SY-1365) 纯度: 99.27%

Mevociclib (SY-1365) 是一种高效、首创、选择性的 CDK7 抑制剂,其 Ki 值为 17.4 nM。Mevociclib 在实体肿瘤细胞系中具有抗增殖和凋亡活性。Mevociclib 具有抗血液肿瘤和侵袭性实体肿瘤作用。

Mevociclib(Synonyms: SY-1365)

Mevociclib Chemical Structure

CAS No. : 1816989-16-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4520 In-stock
5 mg ¥3500 In-stock
10 mg ¥6500 In-stock
50 mg ¥20000 In-stock
100 mg ¥35000 In-stock
200 mg   询价  
500 mg   询价  

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Mevociclib 相关产品

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生物活性

Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors[1][2].

IC50 & Target[1]

CDK7

 

体外研究
(In Vitro)

Mevociclib exhibits inhibition for CDK7/CycH/MAT1 with an IC50 of 20 nM[2].
Mevociclib is a highly selective covalent CDK7 inhibitor, induces apoptosis in leukemia cells, but not in non-malignant cells[2].
Mevociclib exhibits activity in breast, ovarian, colorectal and lung cancer cells that exhibited low nM EC50 and rapid induction of apoptosis[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)

Mevociclib (20mg/kg; i.v.; biw; for 35 days) inhibits tumor growth in TNBC in vivo models[2].
Mevociclib induces unique transcriptional signature[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: Mice, HCC70 xenograft model[2]
Dosage: 20 mg/kg
Administration: Intravenous injection, twice weekly, for 35 days
Result: Inhibited tumor volume in vivo.

Clinical Trial

分子量

587.12

Formula

C31H35ClN8O2

CAS 号

1816989-16-8

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 : 125 mg/mL (212.90 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7032 mL 8.5161 mL 17.0323 mL
5 mM 0.3406 mL 1.7032 mL 3.4065 mL
10 mM 0.1703 mL 0.8516 mL 1.7032 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: ≥ 2.08 mg/mL (3.54 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.54 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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% corn oil

    Solubility: ≥ 2.08 mg/mL (3.54 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.54 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 20.8 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]. Hu S, et al. Discovery and characterization of SY-1365, a selective, covalent inhibitor of CDK7. Cancer Res. 2019 May 7.

    [2]. Shanhu Hu, et al. SY-1365, a potent and selective CDK7 inhibitor, exhibits promising anti-tumor activity in multiple preclinical models of aggressive solid tumors.

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