KRAS inhibitor-10 selectively and effectively inhibitRASproteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used forcancerresearch, such as pancreaticcancer, breastcancer, multiple myeloma, leukemia and lungcancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1^[1].

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^G12Soncogenic mutation), H358 (non-small cell lung cancer line bearing KRas^G12Concogenic mutation), PANC-1 (epithelioid carcinoma of the pancreas cell line bearing KRas^G12Doncogenic mutation) and RPMI (myeloma cell line bearing KRas^G12Aoncogenic mutation) cell proliferation with IC₅₀values of 0.2 μM, 0.2 μM, 0.1 μM and 0.8 μM, respectively^[1].
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 IC₅₀value is 0.413 μM^[1].

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^[1].

519.63

Solid

C₃₀H₃₇N₃O₅

2578876-75-0

Room temperature in continental US; may vary elsewhere.

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

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

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。