CH6953755|cas:2055918-71-1|西域试剂

CH6953755,98.03%

产品编号：Bellancom-135299| CAS NO：2055918-71-1| 分子式：C₂₆H₂₂F₂N₆O₄S| 分子量：552.55

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-135299		￥6000.00	杭州北京（现货）
Bellancom-135299		￥9500.00	杭州北京（现货）

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CH6953755

产品介绍

CH6953755 是一种有效的，具有口服活性和选择性的 YES1 激酶 (SRC 家族的成员)抑制剂，IC₅₀ 为 1.8 nM。CH6953755 通过抑制 YES1 激酶，从而在体内外对 YES1 基因扩增的癌症产生抗肿瘤活性。

生物活性

CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC₅₀ of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo.

体外研究

CH6953755 (0.001-1 μM; for 4 days) inhibits the cell growth of YES1-amplified cancer cell lines.
CH6953755 (0.001-1 μM; for 2 hours) prevents the autophosphorylation at Tyr426 of YES1 that upregulates enzymatic activity in KYSE70 cells harboring YES1 amplification.
CH6953755 (0.1, 0.3, 1, 3 μM) suppresses TEAD luciferase reporter activity in YES1-amplified KYSE70 and RERF-LC-AI.

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

Cell Viability Assay

Cell Line:	YES1-amplified cancer cell lines KYSE70 and OACP4 C, and non-YES1–amplified cancer cell line K562 expressing YES1-WT or YES1-GK
Concentration:	0.001, 0.01, 0.1, 1 μM
Incubation Time:	4 days
Result:	Inhibited the cell growth of YES1-amplified cancer cell lines.

Western Blot Analysis

Cell Line:	KYSE70 cell line
Concentration:	0.001, 0.003, 0.01, 0.03, 0.1, 0.3, 1 μM
Incubation Time:	2 hours
Result:	Prevented the autophosphorylation at Tyr426 of YES1 that upregulates enzymatic activity in KYSE70 cells harboring YES1 amplification

体内研究
(In Vivo)

CH6953755 (oral; 60 mg/kg/day; for 10 days) shows selective antitumor activity accompanied with phospho-Tyr426 YES1 suppression in xenograft tumors.
CH6953755 (oral; 7.5, 15, 30, 60 mg/kg) suppresses phospho-Tyr426 YES1 in a dose-dependent manner.

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

Animal Model:	Female BALB/c-nu/nu mice with Rat-2_YES1 xenograft
Dosage:	60 mg/kg
Administration:	Oral; daily; for 10 days
Result:	Showed selective antitumor activity accompanied with phospho-Tyr426 YES1 suppression in xenograft tumors.

体内研究

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

Animal Model:	Female BALB/c-nu/nu mice with Rat-2_YES1 xenograft
Dosage:	60 mg/kg
Administration:	Oral; daily; for 10 days
Result:	Showed selective antitumor activity accompanied with phospho-Tyr426 YES1 suppression in xenograft tumors.

体内研究

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

Animal Model:	Female BALB/c-nu/nu mice with Rat-2_YES1 xenograft
Dosage:	60 mg/kg
Administration:	Oral; daily; for 10 days
Result:	Showed selective antitumor activity accompanied with phospho-Tyr426 YES1 suppression in xenograft tumors.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (226.22 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8098 mL	9.0490 mL	18.0979 mL
5 mM	0.3620 mL	1.8098 mL	3.6196 mL
10 mM	0.1810 mL	0.9049 mL	1.8098 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 (3.76 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.76 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% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.76 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.76 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 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: ≥ 2.08 mg/mL (3.76 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.76 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。