2. KRAS G12C-IN-77

KRAS G12C-IN-77 是一种具有口服活性和选择性的 KRASG12C 共价双态抑制剂，可以高亲和力与 GDP 结合 (非活性态) 和 GTP 结合 (IC50 = 133 nM) (活性态) 的 KRASG12C 结合。KRAS G12C-IN-77 可快速抑制 ERK1/2 磷酸化，诱导与内源性 KRASG12C 形成共价加合物，抑制 MAPK 通路基因的表达，并抑制 KRASG12C 突变细胞的增殖。KRAS G12C-IN-77 可用于 KRASG12C 突变实体瘤的相关研究，包括胰腺导管腺癌和非小细胞肺癌。

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KRAS G12C-IN-77

KRAS G12C-IN-77 Chemical Structure

CAS No. : 3023465-19-9

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KRAS G12C-IN-77 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KRAS G12C-IN-77 is an orally active and selective KRASG12C covalent dual-state inhibitor that binds with high affinity to both GDP-bound (inactive state) and GTP-bound (active state) KRASG12C (IC50 = 133 nM). KRAS G12C-IN-77 rapidly inhibits ERK1/2 phosphorylation, induces the formation of covalent adducts with endogenous KRASG12C, suppresses the expression of MAPK pathway genes, and inhibits the proliferation of KRASG12C-mutant cells. KRAS G12C-IN-77 is applicable to research related to KRASG12C-mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer[1].

体外研究
(In Vitro)

KRAS G12C-IN-77 (Compound 8) 对 G12C 突变细胞的 IC50 <10 nM，对非 G12C 突变细胞的 IC50 >1000 nM[1]。
KRAS G12C-IN-77 以 0.4 nM 的 IC50 抑制 MIA PaCa-2 KRASG12C 突变细胞中 ERK1/2 的磷酸化[1]。
KRAS G12C-IN-77 (5 days) 强效抑制 MIA PaCa-2 KRASG12C 突变细胞的增殖，IC50 为 1.6 nM[1]。

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

KRAS G12C-IN-77 相关抗体:
体内研究
(In Vivo)

KRAS G12C-IN-77 (Compound 8) (5-150 mg/kg；口服；每日一次；连续 21 天) 可在 MIA PaCa-2 异种移植瘤小鼠中诱导深度肿瘤消退[1]。
KRAS G12C-IN-77 (150 mg/kg；口服；每日 2 次；连续 21 天) 在 LUN-055 KRASG12C 异种移植模型中可诱导 88% 的肿瘤生长抑制，同时实现强效的靶点结合与通路抑制[1]。

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

Animal Model: Crl:NU(NCr)-Foxn1^nu homozygous nude mice (female, 6-8 weeks old, implanted with MIA PaCa-2 KRAS G12C mutant cells)[1]
Dosage: 5, 15, 50, 150 mg/kg
Administration: p.o.; single dose; daily; 21 days
Result: Achieved over 85% KRAS G12C covalent engagement and approximately 50% pERK suppression at 1 hour post 50 mg/kg and 150 mg/kg single dose relative to vehicle.
Reached maximum target engagement (over 90% at 150 mg/kg) with sustained pERK suppression by 7 hours post all single doses.
Induced significant tumor growth inhibition at 15 mg/kg, 50 mg/kg, and 150 mg/kg after 21 days of daily dosing.
Drove complete tumor responses in 6 of 8 animals (75%) with tumor volumes remaining near baseline at 150 mg/kg daily dose for 21 days.
Animal Model: BALB/c nude mice (female, 6-8 weeks old, implanted with LUN-055 KRAS G12C mutant tumor fragments)[1]
Dosage: 150 mg/kg
Administration: p.o.; twice daily; 21 days
Result: Achieved 88% tumor growth inhibition relative to vehicle.
Reached high levels of KRAS G12C target engagement and significant pERK suppression measured 7 hours after the final dose.
分子量

689.73

Formula

C39H34F3N7O2
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

KRAS G12C-IN-77 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:

KRAS G12C-IN-773023465-19-9GMPPNPGDPKRAS G12Cmouse xenograft modelsnon-small cell lung cancerH1373 cellspancreatic ductal adenocarcinomaMAPK pathwayRAF RBDERK1/2Inhibitorinhibitorinhibit

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