2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. KRASG12C IN-18

KRASG12C IN-18 是一种口服活性的 KRASG12C 共价抑制剂，可在 GDP 与 GMPPNP 结合状态下实现对 KRASG12C 的完全共价结合，并对 KRASG12C 及其耐药相关突变体（包括 KRASG12C/R68S）表现出显著的抗增殖活性，IC50 为低纳摩尔水平。 KRASG12C IN-18 在 KRASG12C 驱动的实体瘤及 KRASG12C/R68S 异种移植模型中表现出显著的体内活性，可用于直肠腺癌研究。

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KRASG12C IN-18

KRASG12C IN-18 Chemical Structure

CAS No. : 2966924-24-1

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KRASG12C IN-18 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KRASG12C IN-18 is an orally active covalent KRASG12C inhibitor that achieves complete covalent engagement of KRASG12C in both GDP- and GMPPNP-bound states and displays strong antiproliferative activity against KRASG12C and resistance-associated variants, including KRASG12C/R68S, with low-nanomolar IC50 values. KRASG12C IN-18 exhibits marked in vivo efficacy in KRASG12C-driven solid tumor and KRASG12C/R68S xenograft models and can be used for colorectal cancer research[1].

IC50 & Target[1]

KRAS(G12C)

 

体外研究
(In Vitro)

在 72-144 h 处理条件下，KRASG12C IN-18 可显著抑制 KRASG12C 突变的 Ba/F3 细胞及多种次级耐药突变体，包括 H95Q (IC50 = 7.5 nM)、Y96D (IC50 = 2.8 nM)、R68S (IC50 = 5.4 nM) 和 Q99L (IC50 = 8.2 nM)，在上述模型中均表现出低纳摩尔级抑制活性[1]。
KRASG12C IN-18 可在 GDP 与 GMPPNP 状态下快速且高效地实现对 KRASG12C 的 100% 共价修饰[1]。

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

KRASG12C IN-18 相关抗体:
体内研究
(In Vivo)

KRASG12C IN-18 (SW837 KRASG12C 直肠癌异种移植模型；口服给药，30 mg/kg，每日一次，28 天) 表现出显著的抗肿瘤活性，实现 103% 的肿瘤生长抑制，且优于 MRTX849 与 AMG 510[1]。 KRASG12C IN-18 (Ba/F3 KRASG12C/R68S 异种移植模型；口服给药，30 mg/kg，每日一次，21 天) 同样表现出显著的抗肿瘤活性，可引起 79.2% 的肿瘤回缩，并具有良好的耐受性[1]。

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

Animal Model: SW837 human rectal cancer xenograft (KRASG12C) female NOD SCID mice (6–7 weeks old, 20.5-23.7 g)
Dosage: 30 mg/kg
Administration: Oral gavage (p.o.); once daily; 28 days
Result: Achieved 103% tumor growth inhibition and induced complete tumor stasis without body-weight loss.
Animal Model: Ba/F3 KRASG12C/R68S xenograft model female NOD SCID mice (6-8 weeks old, 18.6-23.3 g)
Dosage: 30 mg/kg
Administration: Oral gavage (p.o.); once daily; 21 days
Result: Produced 79.2% tumor regression and demonstrated good tolerability.
分子量

668.68

Formula

C37H32F4N6O2
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-18 相关分类

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  • 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-182966924-24-1RasKRAS G12Ccovalent inhibitorresistance mutationR68Sxenograftconjugation efficiencycolorectal cancerInhibitorinhibitorinhibit

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