Samuraciclib hydrochloride CT7001 hydrochloride; ICEC0942 hydrochloride|cas:1805789-54-1|西域试剂

Samuraciclib hydrochloride CT7001 hydrochloride; ICEC0942 hydrochloride,98.80%

产品编号：Bellancom-103712A| CAS NO：1805789-54-1| 分子式：C₂₂H₃₁ClN₆O| 分子量：430.97

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-103712A	￥2500.00	杭州北京（现货）
Bellancom-103712A	￥4200.00	杭州北京（现货）
Bellancom-103712A	￥8600.00	杭州北京（现货）
Bellancom-103712A	￥14000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Samuraciclib hydrochloride CT7001 hydrochloride; ICEC0942 hydrochloride

产品介绍

Samuraciclib hydrochloride (CT7001 hydrochloride) 是一种有效的，具有选择性，ATP 竞争性和口服活性的 CDK7 抑制剂，IC₅₀ 为 41 nM。Samuraciclib hydrochloride 对 CDK7 的选择性分别是 CDK1，CDK2 (IC₅₀ 为 578 nM)，CDK5 和 CDK9 的 45 倍，15 倍，230 倍和 30 倍。Samuraciclib hydrochloride 以 GI₅₀ 值为 0.2-0.3 µM 来抑制乳腺癌细胞系的生长，具有有效的抗肿瘤作用。

生物活性

Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC₅₀ of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC₅₀ of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI₅₀ values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects.

体外研究

Samuraciclib (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment promotes cell apoptosis.
Samuraciclib (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment induces cell cycle arrest.
Samuraciclib (ICEC0942; 0-10 µM; 0-24 hours; HCT116 cells) treatment inhibits the phosphorylation of PolII CTD in a dose and time dependent manner in HCT116 colon cancer cells. ICEC0942 also inhibits phosphorylation of CDK1, CDK2 and retinoblastoma.
Samuraciclib (ICEC0942) inhibits the growth of MCF7, T47D, MDA-MB-231, HS578T, MDA-MB-468, MCF10A and HMEC cells with GI₅₀ values of 0.18 µM, 0.32 µM, 0. 33 µM, 0.21 µM, 0.22 µM, 0.67 µM and 1.25 µM, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis

Cell Line:	HCT116 cells
Concentration:	0 µM, 0.1 µM, 1 µM and 10 µM
Incubation Time:	24 hours
Result:	Induced caspase 3/7 and demonstrated PARP cleavage.

Cell Cycle Analysis

Cell Line:	HCT116 cells
Concentration:	0 µM, 0.01 µM, 0.1 µM, 1 µM and 10 µM
Incubation Time:	24 hours
Result:	Showed accumulation of cells in G2/M.

Western Blot Analysis

Cell Line:	HCT116 cells
Concentration:	0 µM, 0.1 µM, 1 µM and 10 µM
Incubation Time:	0 hour, 4 hours, 8 hours, 16 hours or 24 hours
Result:	PolII CTD phosphorylation was inhibited in a dose and time dependent manner in HCT116 colon cancer cells.

体内研究
(In Vivo)

Samuraciclib (ICEC0942; 100 mg/kg; oral gavage; daily; for 14 days; female nu/nu-BALB/c athymic nude mice) treatment inhibits tumor growth by 60% at day 14, and is accompanied by highly significant reductions in PolII Ser2 and Ser5 phosphorylation in PBMCs and in tumors.
The combination of Samuraciclib (ICEC0942) and ICI 47699 treatment shows complete growth arrest of estrogen receptor (ER)-positive tumor xenografts.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female nu/nu-BALB/c athymic nude mice (7-week old) with MCF7 cells
Dosage:	100 mg/kg
Administration:	Oral gavage; daily; for 14 days
Result:	At day 14, tumor growth was inhibited by 60%.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female nu/nu-BALB/c athymic nude mice (7-week old) with MCF7 cells
Dosage:	100 mg/kg
Administration:	Oral gavage; daily; for 14 days
Result:	At day 14, tumor growth was inhibited by 60%.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female nu/nu-BALB/c athymic nude mice (7-week old) with MCF7 cells
Dosage:	100 mg/kg
Administration:	Oral gavage; daily; for 14 days
Result:	At day 14, tumor growth was inhibited by 60%.

性状

Solid

溶解性数据

In Vitro:

H₂O : 55 mg/mL (127.62 mM; Need ultrasonic)

DMSO : 50 mg/mL (116.02 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3203 mL	11.6017 mL	23.2035 mL
5 mM	0.4641 mL	2.3203 mL	4.6407 mL
10 mM	0.2320 mL	1.1602 mL	2.3203 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 (stored under nitrogen, away from moisture)。-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： PBS
Solubility: 100 mg/mL (232.03 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.80 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.80 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
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.80 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.80 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
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.80 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.80 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。