1. GPCR/G Protein
    Apoptosis
  2. Ras
    Apoptosis
  3. KRAS inhibitor-9

KRAS inhibitor-9 

目录号: HY-137497 纯度: 99.98%
产品使用指南

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

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

KRAS inhibitor-9 Chemical Structure

KRAS inhibitor-9 Chemical Structure

CAS No. : 300809-71-6

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

Size Price Stock Quantity
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   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Top Publications Citing Use of Products

View All Ras Isoform Specific Products:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

Description

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].

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].

MCE 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.
Molecular Weight

292.81

Formula

C₁₃H₉ClN₂S₂

CAS No.

300809-71-6

SMILES

NC1=CC=C(SC2=NC3=CC=CC=C3S2)C(Cl)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (853.80 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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 MCE 网站选购。
References
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

KRAS inhibitor-9KRAS inhibitor9KRAS inhibitor 9RasApoptosisnon-smallcelllungcancercellscytotoxicityproliferationGTP-KRASmutantH2122H358H460Inhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称:

 

* 需求量:

* 客户姓名:

 

* Email:

* 电话:

 

* 公司或机构名称:

   留言给我们:

Bulk Inquiry

Inquiry Information

产品名称:
KRAS inhibitor-9
目录号:
HY-137497
需求量: