2. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease MAPK/ERK Pathway Stem Cell/Wnt
  3. Reactive Oxygen Species (ROS) ERK
  4. KRASG12C IN-19

KRASG12C IN-19 是一种选择性 KRASG12C 抑制剂。KRASG12C IN-19 对 KRASG12C 突变型非小细胞肺癌 (NSCLC) 细胞系 H358 展现出强效的抗增殖活性 (IC50 = 7.6 nM) ，并能有效抑制下游 ERK 磷酸化 (IC50 = 24.06 nM)。KRASG12C IN-19 对 KRASG12V 及 KRASG12D 突变型癌细胞 (PANC 1、Panc 03.27、AsPC 1 和 GP2d 细胞) 无显著抑制活性 (IC50 > 10,000 nM)。KRASG12C IN-19 能快速与 KRASG12V-GDP 形成共价键，从而实现对下游 KRAS 通路的剂量依赖性抑制。KRASG12C IN-19 可用于 KRASG12C 驱动的癌症研究，包括非小细胞肺癌、胰腺癌和结直肠癌。

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KRASG12C IN-19

KRASG12C IN-19 Chemical Structure

CAS No. : 2915282-32-3

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KRASG12C IN-19 相关抗体

Top Publications Citing Use of Products

查看 ERK 亚型特异性产品:

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ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KRASG12C IN-19 is a selective and orally active KRASG12C inhibitor. KRASG12C IN-19 exerts potent antiproliferative activity against the KRASG12C-mutant non small cell lung cancer (NSCLC) cell line H358 with an IC50 of 7.6 nM, and effectively suppresses downstream ERK phosphorylation (IC50 = 24.06 nM). KRASG12C IN 19 has no significant inhibitory activity against KRASG12V and KRASG12D-mutant cancer cells (PANC 1, Panc, AsPC 1, and GP2d cells) with IC50 > 10,000 nM. KRASG12C IN-19 rapidly forms a covalent bond with KRASG12V-GDP, leading to dose-dependent inhibition of the downstream KRAS pathway. KRASG12C IN 19 can be employed for research in KRASG12C driven cancers, including non small cell lung cancer, pancreatic cancer, and colorectal cancer[1].

IC50 & Target[1]

ERK

24.6 nM (IC50)

体外研究
(In Vitro)

KRASG12C IN-19 (compound 8t) 在人源和小鼠肝微粒体中表现出优异的代谢稳定性 (半衰期 T1/2 分别为 188.2 和 112.3 分钟，固有清除率 CLint 分别为 6.4 和 15.8 mL/min/kg) [1]。
KRASG12C IN-19 (4.88-312.5 nM，处理 72 小时) 对 H358 非小细胞肺癌细胞 表现出显著的纳摩尔级抗增殖活性，其 IC50 值为 7.6 nM[1]。
KRASG12C IN-19 (4.88-312.5 nM，处理 72 小时) 对 PANC-1 (IC50 > 1000 nM，KRASG12V 突变细胞)、Panc 03.27 (IC50 > 1000 nM)、AsPC-1 (IC50 > 1000 nM，KRASG12D 突变细胞) 和 GP2d (IC50 > 1000 nM) 癌细胞未显示出细胞抑制效力[1]。
KRASG12C IN-19 (4.88-312.5 nM，处理 3 小时) 在 H358 细胞上剂量依赖性地抑制 ERK 磷酸化，其 IC50 为 24.06 nM[1]。
KRASG12C IN-19 在 KRASG12C 突变型 H358 细胞中抑制 ERK 磷酸化[1]。
KRASG12C IN-19 (4.88-312.5 nM) 对 hERG 通道的毒性潜力低，在 CHO 细胞系中的 IC50 > 30 μM[1]。

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

KRASG12C IN-19 相关抗体:
体内研究
(In Vivo)

KRASG12C IN-19 (30 mg/kg，口服给药，每日一次，连续 29 天) 可在雌性 BALB/c 小鼠体内显著抑制携带 KRASG12C 突变的人源 H358 NSCLC 细胞衍生异种移植瘤的生长，且未引发可观察到的毒副作用[1]。

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

Animal Model: Human H358 NSCLC cell-derived xenograft tumors bearing the KRASG12C mutation in female BALB/c mice (5-6 weeks old)[1]
Dosage: 30 mg/kg
Administration: p.o., once daily for 29 days
Result: Enhanced tumor regression, achieving a tumor growth inhibition (TGI) rate of 167.9 %.
Observed no notable changes in body weight.
分子量

590.65

Formula

C33H31FN8O2
CAS 号
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-19 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

KRASG12C IN-192915282-32-3Reactive Oxygen Species (ROS)ERKExtracellular signal regulated kinasesnon small cell lung cancerpancreatic cancerand colorectal cancerKRASG12C,ERKInhibitorinhibitorinhibit

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