2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. KRASG12C IN-20

KRASG12C IN-20 是一种口服有效的 KRASG12C 抑制剂，EC50 为 3.9 nM。KRASG12C IN-20 可共价修饰处于非活性 GDP 结合状态的 KRASG12C，将其锁定以阻断致癌信号传导。KRASG12C IN-20 在肺腺癌异种移植模型中具有显著活性。KRASG12C IN-20 可用于肺腺癌的相关研究。

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KRASG12C IN-20

KRASG12C IN-20 Chemical Structure

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KRASG12C IN-20 相关抗体

Top Publications Citing Use of Products

查看 Ras 亚型特异性产品:

查看所有亚型
K-Ras H-Ras N-Ras Ras

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KRASG12C IN-20 is an orally potent KRASG12C inhibitor with an EC50 of 3.9 nM. KRASG12C IN-20 covalently modifies KRASG12C in its inactive GDP-bound state and locks it to block oncogenic signal transduction. KRASG12C IN-20 exhibits significant activity in lung adenocarcinoma xenograft models. KRASG12C IN-20 can be used for research related to lung adenocarcinoma[1].

IC50 & Target[1]

KRAS(G12C)

3.9 nM (EC50)

体外研究
(In Vitro)


KRASG12C IN-20 (Compoud 13de) 可强效且选择性地抑制 H358 KRASG12C 人肺腺癌细胞的增殖，其 EC50 为 3.9 nM[1]。

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

KRASG12C IN-20 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route CL Vss Bioavailability
Mice[1] 2 mg/kg i.v. 43.9 mL/min/kg 2.7 L/kg 13.5 %
Mice[1] 10 mg/kg p.o. / / 13.5 %
Rat[1] 2 mg/kg i.v. 94.6 mL/min/kg 11.4 L/kg 4 %
Rat[1] 10 mg/kg p.o. / / 4 %
Dog[1] 1 mg/kg i.v. 91.5 mL/min/kg 12.8 L/kg 10.9 %
Dog[1] 5 mg/kg p.o. / / 10.9 %
Monkey[1] 1 mg/kg i.v. 144 mL/min/kg 18 L/kg 3.6 %
Monkey[1] 5 mg/kg p.o. / / 3.6 %
体内研究
(In Vivo)

KRASG12C IN-20 (Compoud 13de) (1-15 mg/kg；口服；每日 1 次；28 天) 在 NCI-H1373 异种移植模型中表现出强效的剂量依赖性肿瘤生长抑制作用[1]。
KRASG12C IN-20 (5-10 mg/kg；口服；每日 1 次；连续 3 天) 在 NCI-H1373 异种移植模型中可在 24 h 内实现持续、强效的瘤内 KRASG12C-GDP 靶点结合[1]。

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

Animal Model: athymic nude (female)[1]
Dosage: 1 mg/kg; 5 mg/kg; 15 mg/kg
Administration: p.o.; QD; 28 days
Result: Achieved a ΔTGI of 108% at 5 mg/kg QD compared to vehicle-treated controls.
Achieved a ΔTGI of 109% at 15 mg/kg QD compared to vehicle-treated controls.
Showed minimal antitumor activity at 1 mg/kg QD.
Animal Model: athymic nude (female)[1]
Dosage: 5 mg/kg; 10 mg/kg
Administration: p.o.; QD; 3 days
Result: Elicited robust intratumoral KRASG12C-GDP target engagement at 5 mg/kg QD, with high engagement levels maintained at 24 h post-final dose.
Elicited robust intratumoral KRASG12C-GDP target engagement at 10 mg/kg QD, with high engagement levels maintained at 24 h post-final dose.
分子量

674.72

Formula

C35H37F3N8O3
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

KRASG12C IN-20 相关分类

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  • 稀释计算器

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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.

Keywords:

KRASG12C IN-20Rastumor growthKRASG12C-GDPKRASG12Clung adenocarcinomaH358 KRASG12C human lung adenocarcinoma cellsNCI-H1373 xenograft modeloncogenic signalingInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-182883
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