1. GPCR/G Protein MAPK/ERK Pathway
  2. Ras
  3. KRAS G12C inhibitor 65

KRAS G12C inhibitor 65 是一种有效的 KRASG12C 共价抑制剂,可将 KRASG12C 捕获在 GDP 结合状态。KRAS G12C inhibitor 65 对 KRAS 突变型非小细胞肺癌具有有效的抗肿瘤活性。

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KRAS G12C inhibitor 65 Chemical Structure

KRAS G12C inhibitor 65 Chemical Structure

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Customer Review

查看 Ras 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KRAS G12C inhibitor 65 is a potent and covalent KRASG12C inhibitor that traps KRASG12C in the GDP-bound state. KRASG12C IN-1 exhibits potent antitumor activity against KRAS-mutant non-small cell lung cancer[1].

体外研究
(In Vitro)

KRAS G12C inhibitor 65 (compound 20a) (72 h) shows potent and selective antiproliferative activities against KRASG12C NSCLC cells, with IC50s of 0.5 μM against NCI-H358 cells and 1.30 μM against NCI-H23 cells, with 7- to 21-fold selectivity over KRASG12S and KRASWT cells[1].
KRAS G12C inhibitor 65 (0.5-8.0 μM; 6 h) decreases the phosphorylation of ERK and AKT in KRASG12C-mutant NCIH358 cells[1].

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

Western Blot Analysis[1]

Cell Line: NCI-H358 and NCI-H2228 cells
Concentration: 0.5, 1.0, 2.0, 4.0, 8.0 μM
Incubation Time: 6 hours
Result: Showed no impact on KRAS signaling in KRASWT NCI-H2228 cells.
The pERK level decreased 40%-90%, and the pAKT level was down-regulated by 30%-90% in NCI-H358 cells.
体内研究
(In Vivo)

KRAS G12C inhibitor 65 (compound 20a) (10-15 mg/kg; i.p. every 2 d for 21 d) inhibited tumor growth in H358 xenografts by suppressing KRASG12C signalling[1].

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

Animal Model: Female BALB/c Nude mice were injected subcutaneously with NCI-H358 cells[1]
Dosage: 10, 15 mg/kg
Administration: I.p. every two days for 21 days
Result: Significantly inhibited tumor growth while the body weight of mice was not influenced.
分子量

410.27

Formula

C19H18Cl2FN3O2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
KRAS G12C inhibitor 65
目录号:
HY-151999
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