KRAS inhibitor-10|cas:2578876-75-0|西域试剂

KRAS inhibitor-10,99.86%

产品编号：Bellancom-138295| CAS NO：2578876-75-0| 分子式：C₃₀H₃₇N₃O₅| 分子量：519.63

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-138295		￥4500.00	杭州北京（现货）
Bellancom-138295		￥8000.00	杭州北京（现货）

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KRAS inhibitor-10

产品介绍

KRAS inhibitor-10 选择性有效抑制 RAS 蛋白，特别是 KRAS 蛋白。KRAS inhibitor-10 是一种口服活性抗癌化合物，可用于癌症研究，如胰腺癌、乳腺癌、多发性骨髓瘤、白血病和肺癌。KRAS inhibitor-10 是一种四氢异喹啉化合物 (化合物 11)，详细信息请参考专利 WO2021005165 A1。

生物活性

KRAS inhibitor-10 selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1.

体外研究

KRAS inhibitor-10 (0.1-50 µΜ; 72 hours) has antiproliferative effects in KRas mutant tumor cells, KRAS inhibitor-10 is against A549 (lung carcinoma cell line bearing KRas^G12S oncogenic mutation), H358 (non-small cell lung cancer line bearing KRas^G12C oncogenic mutation), PANC-1 (epithelioid carcinoma of the pancreas cell line bearing KRas^G12D oncogenic mutation) and RPMI (myeloma cell line bearing KRas^G12A oncogenic mutation) cell proliferation with IC₅₀ values of 0.2 μM, 0.2 μM, 0.1 μM and 0.8 μM, respectively.
KRAS inhibitor-10 (0-1 μM, 7 days) is against cell viability in a 3D CellTiter-GloTM cell viability assay for NIH-H358 cell, the IC₅₀ value is 0.413 μM.

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

体内研究

KRAS inhibitor-10 (oral administration; 20 mg/kg; BID; 27 days) is safe and tolerate for the bearing mice. KRAS inhibitor-10 demonstrates significant oral anti-tumor activities in vivo. And the tumor growth inhibition (TGI) value is 48.22% for KRAS inhibitor-10.

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

Animal Model:	Subcutaneous NCI-H358 Human Lung Cancer Model in NCr nude mice
Dosage:	20 mg/kg
Administration:	Oral administration; 20 mg/kg; BID; 27 days
Result:	Decreased tumor volume and exhibited anti-tumor effects in the bearing mice.

体内研究

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

Animal Model:	Subcutaneous NCI-H358 Human Lung Cancer Model in NCr nude mice
Dosage:	20 mg/kg
Administration:	Oral administration; 20 mg/kg; BID; 27 days
Result:	Decreased tumor volume and exhibited anti-tumor effects in the bearing mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (192.44 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9244 mL	9.6222 mL	19.2445 mL
5 mM	0.3849 mL	1.9244 mL	3.8489 mL
10 mM	0.1924 mL	0.9622 mL	1.9244 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 (4.81 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.81 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% corn oil
Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.81 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。