KRAS inhibitor-9

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KRAS inhibitor-9  纯度: 99.98%

KRAS inhibitor-9 是有效的 KRAS 抑制剂 (Kd=92 μM)，阻止 GTP-KRAS 的形成和 KRAS 下游激活。KRAS inhibitor-9 以中等的结合亲和力与 KRAS G12D，KRAS G12C 和 KRAS Q61H 蛋白结合。KRAS inhibitor-9 导致 G2/M 细胞周期停滞并诱导凋亡 (apoptosis)。KRAS inhibitor-9 选择性抑制具有 KRAS 突变的 NSCLC 细胞的增殖，但不抑制正常肺细胞的增殖。KRAS inhibitor-9

KRAS inhibitor-9

KRAS inhibitor-9 Chemical Structure

CAS No. : 300809-71-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1650 In-stock
5 mg ￥1500 In-stock
10 mg ￥2500 In-stock
25 mg ￥4500 In-stock
50 mg ￥6500 In-stock
100 mg ￥8500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells[1].

体外研究
(In Vitro)

KRAS inhibitor-9 bound to KRASG12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity of -5.38, -5.41, and -3.97 kcal/mol, respectively[1].
KRAS inhibitor-9 (0-100 μM) shows strong inhibition selectivity in NSCLC cells with IC50s ranging from 39.56 to 66.02 μM for H2122, H358 and H460 cells (at 72 hours)[1].
KRAS inhibitor-9 (0-100 μM; 24 hours) blocks GTP-KRAS formation in H2122, H358 and H460 cells[1].
KRAS inhibitor-9 (25-100 μM; 48 hours) inhibits the activation of KRAS downstream signaling pathway[1].
KRAS inhibitor-9 (0-100 μM; 24-72 hours) induces cell cycle arrest and apoptosis in NSCLC[1].

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.

Cell Viability Assay[1]

Cell Line: H2122 (KRAS G12C), H358 (KRAS G12C) and H460 (KRAS Q61H) cell lines
Concentration: 0, 25, 50, 100 μM
Incubation Time: 24, 48, and 72 hours
Result: Inhibited three NSCLC cell lines in a dose- and time-dependent manner, but not in normal lung fibroblast cell line CCD-19Lu.

Western Blot Analysis[1]

Cell Line: H2122, H358 and H460 cells
Concentration: 0, 25, 50, 100 μM
Incubation Time: 48 hours
Result: Reduces the levels of phosphorylation of CRAF and AKT in a dose-dependent manner in H2122, H358 and H460 cells.

Apoptosis Analysis[1]

Cell Line: H2122, H358, H460 cells
Concentration: 0, 25, 50, 100 μM
Incubation Time: 24-72 hours
Result: Significantly decreased in G0/G1 phase while remarkably increased in G2/M phase after 24 hours and induced a significantly increased apoptosis for 48h in NSCLC cell lines.

分子量

292.81

Formula

C13H9ClN2S2
CAS 号

300809-71-6
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 : 250 mg/mL (853.80 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.4152 mL 17.0759 mL 34.1518 mL
5 mM 0.6830 mL 3.4152 mL 6.8304 mL
10 mM 0.3415 mL 1.7076 mL 3.4152 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    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (7.10 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.10 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
  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (7.10 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.10 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]. Xie C, et al. Identification of a New Potent Inhibitor Targeting KRAS in Non-small Cell Lung Cancer Cells. Front Pharmacol. 2017;8:823. Published 2017 Nov 14.

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