2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. KRAS G12C inhibitor 57

KRAS G12C inhibitor 57 (Compound 50) 是一种有效的、选择性的、共价的和具有口服活性的 KRAS G12C 抑制剂，在 KRAS G12C/SOS1 结合试验中对 KRAS G12C 的 IC50 为 0.21 μM。KRAS G12C inhibitor 57 诱导癌细胞凋亡 (apoptosis)。

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KRAS G12C inhibitor 57 Chemical Structure

KRAS G12C inhibitor 57 Chemical Structure

CAS No. : 2821863-70-9

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KRAS G12C inhibitor 57 相关抗体

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  • 生物活性

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  • 参考文献

生物活性

KRAS G12C inhibitor 57 (Compound 50) is a potent, selective, covalent and orally active KRAS G12C inhibitor with an IC50 of 0.21 μM in KRAS G12C/SOS1 binding assay. KRAS G12C inhibitor 57 induces cancer cell apoptosis[1].

IC50 & Target[1]

KRAS(G12C)

0.21 μM (IC50, KRAS G12C/SOS1 binding assay)

体外研究
(In Vitro)

KRAS G12C inhibitor 57 (Compound 50) (0-10 μM; 3 days) 对 KRAS 和 KRAS 驱动的细胞系有选择性抑制，以及对下游信号的强烈抑制[1]。
KRAS G12C inhibitor 57 (0.1-1 μM; 24 h) 诱导 H358 细胞凋亡[1]。
KRAS G12C inhibitor 57 (0.1-1 μM; 48 h) 抑制 H358 细胞肿瘤转移[1]。

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

KRAS G12C inhibitor 57 相关抗体:

Western Blot Analysis[1]

Cell Line: H358 (KRAS p. G12C) cells
Concentration: 0, 0.1, 0.3, 0.5, 1 and 5 μM
Incubation Time: 4 and 24 h
Result: Inhibited the active KRAS-GTP and the phosphorylation of ERK and AKT (MAPK and PI3K pathway) in the dose- and time-dependent manners, and strong inhibitory effects on the phosphorylation of ERK at the concentration of 0.1 μM. Increased the cleaved PARP and caspase-7 induction (24 h).

Western Blot Analysis[1]

Cell Line: H1975 cell line
Concentration: 5, 10, and 20 μM
Incubation Time: 4 h
Result: Interrupted the phosphorylation of ERK.

Cell Proliferation Assay[1]

Cell Line: H358 cells harboring KRAS p.G12C, MIA Paca2 cells harboring KRAS p.G12C, H1975 cells harboring KRAS p.WT and A549 cells harboring KRAS p.G12S
Concentration: 0-10 μM
Incubation Time: 3 days
Result: Displayed favourable inhibitory activities on H358 cells and MIA Paca2 cells with the IC50 values of 0.16 μM and 0.87 μM, in sharp contrast with no obvious inhibition on cell proliferation on H1975 cells (IC50 = 7.91 μM) and A549 cells (IC50 = 29.9 μM).

Apoptosis Analysis[1]

Cell Line: H358 cell line
Concentration: 0.1, 0.3, 0.5 and 1 μM
Incubation Time: 24 h
Result: Induced cellular apoptosis in dose-dependent manner.

Cell Migration Assay [1]

Cell Line: H358 cells
Concentration: 0.1, 0.5 and 1 μM
Incubation Time: 48 h
Result: Significantly suppressed the migration.

Cell Invasion Assay[1]

Cell Line: H358 cells
Concentration: 0.1, 0.5 and 1 μM
Incubation Time: 48 h
Result: Inhibited the cellular invasion and exhibited the dose-dependent inhibitory potency.
体内研究
(In Vivo)

KRAS G12C inhibitor 57 (Compound 50) (10 and 30 mg/kg; p.o.; daily for 20 days) 对 H358异种移植模型小鼠有抗肿瘤作用。
Pharmacokinetic data of KRAS G12C inhibitor 57 (Compound 50) in ICR mice. [1]

Parameter iv (3 mg/kg) Parameter po (30 mg/kg)
AUC(0−t) (h*ng/mL) 801 AUC(0−t) (h*ng/mL) 600
AUC(0−∞) (h*ng/mL) 804 AUC(0−∞) (h*ng/mL) 835
C0 (ng/mL) 1964 Cmax (ng/mL) 316
T1/2 (h) 0.930 T1/2 (h) 4.79
Vss (L/kg) 4.98 Tmax (h) 0.083
CL (mL/h/kg) 3739 F (%) 10.4
AUCo‑inf (h*mg/mL) 7060 ± 1020 (14.5%) 21800 ± 2310 (10.6%) 101000 ± 16700 (16.6%)

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

Animal Model: BALB/c-nu/nu mice, H358 xenograft model[1]
Dosage: 10 mg/kg and 30 mg/kg
Administration: Oral administration, daily for 20 days
Result: Significantly inhibited the tumor growth in a dose-dependent manner with remarkable tumor regression at the dose of 30 mg/kg (tumor growth inhibition, TGI = 84.0%). All dosage groups were well-tolerated with no loss of body weight and no morphological damage to viscera including the heart, spleen, and kidney. Significantly suppressed the phosphorylation of ERK and AKT in tumors of nude mice when dosing orally at 10 mg/kg and 30 mg/kg.
Animal Model: ICR mice[1]
Dosage: 3 mg/kg or 30 mg/kg
Administration: IV or PO (Pharmacokinetic Analysis)
Result: Displayed reasonable clearance and half-life by iv administration. Showed a moderate oral bioavailability (F) of 10.4%.
分子量

607.72

Formula

C35H38FN7O2
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 inhibitor 57 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

KRAS G12C inhibitor 572821863-70-9RasH358H1975MIA Paca2A549BALB/c-nu/nu miceanticancerInhibitorinhibitorinhibit

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