2. GPCR/G Protein MAPK/ERK Pathway Apoptosis
  3. Ras Apoptosis
  4. KRAS G12C-IN-74

KRAS G12C-IN-74 是一种口服有效的、选择性的 KRASG12C 抑制剂，其靶点 IC50 为 43.18 nM。KRAS G12C-IN-74 可在 KRASG12C 突变型癌细胞中诱导 G0/G1 细胞周期阻滞和细胞凋亡 (apoptosis)。KRAS G12C-IN-74 可用于 KRASG12C 突变型胰腺癌、结直肠癌和肺癌的研究。

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KRAS G12C-IN-74

KRAS G12C-IN-74 Chemical Structure

CAS No. : 3085516-79-3

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KRAS G12C-IN-74 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

KRAS G12C-IN-74 is an orally active, selective KRASG12C inhibitor with a target IC50 of 43.18 nM. KRAS G12C-IN-74 induces G0/G1 cell cycle arrest and apoptosis in KRASG12C-mutant cancer cells. KRAS G12C-IN-74 is applicable for the research of KRASG12C-mutant pancreatic cancer, colorectal cancer and lung cancer[1].

IC50 & Target[1]

KRas G12C

43.18 nM (IC50)

体外研究
(In Vitro)

KRAS G12C-IN-74 (Compound 7q) (7 days) 可强效抑制 NCI-H358 3D 细胞球体的增殖，其 IC50 为 0.42 nM[1]。
KRAS G12C-IN-74 (72 h) 可强效抑制 KRASG12C 突变细胞系的增殖，其 IC50 值范围为 0.42 nM (NCI-H358, 3D) 至 3.331 μM (H1373)，而对非 G12C 型 KRAS 突变细胞系及野生型细胞系的活性较弱[1]。
KRAS G12C-IN-74 (200-800 nM; 48 h) 在 NCI-H358 细胞中诱导细胞周期停滞于 G0/G1 期，并诱导细胞凋亡[1]。
KRAS G12C-IN-74 (1-8 μM; 48 h) 可在 NCI-H1373 细胞中诱导剂量依赖性凋亡，且与 ML385 (HY-100523) 或 RBN-2397 (HY-136174) 联合用药后，孵育 48 h 后的凋亡率分别显著提升至 81.28% 和 82.75%[1]。
KRAS G12C-IN-74 (72 h) 与泛 USP 抑制剂 PR-619 (HY-13814) 联合使用后，可将其对固有耐药性 NCI-H1373 细胞的 IC50 从微摩尔级大幅降至纳摩尔级[1]。

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

KRAS G12C-IN-74 相关抗体:

Apoptosis Analysis[1]

Cell Line: NCI-H1373 (KRASG12C mutant, intrinsically resistant) cells
Concentration: 1 μM, 4 μM, 8 μM (alone); 8 μM + 0.2 μM ML385; 8 μM + 0.2 μM RBN-2397
Incubation Time: 48 h
Result: Induced apoptosis in H1373 cells in a dose-dependent manner, with an apoptotic rate of 34% at 8 μM.
Increased the apoptotic rate to 81.28% when combined with 0.2 μM ML385, and to 82.75% when combined with 0.2 μM RBN-2397.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 C0 AUC0-t AUC0-∞ Vd CL MRT0-last Tmax Cmax MRT F
Rat[1] 3 mg/kg i.v. 4.14 h 3319 ng/mL 1286 ng·h/mL 1301 ng·h/mL 13867 mL/kg 2342 mL/h/kg 3.88 h / / / /
Rat[1] 30 mg/kg p.o. 3.14 h / 3112 ng·h/mL 3137 μg·h/mL / / / 3.33 h 359 ng/mL 6.51 h 24.1 %
体内研究
(In Vivo)

KRAS G12C-IN-74 (Compound 7q) (3-30 mg/kg; p.o.; 每日一次共 21 天) 在 MIA PaCa-02 胰腺癌异种移植模型中表现出强效的剂量依赖性抗肿瘤活性[1]。
KRAS G12C-IN-74 (100 mg/kg; p.o.; 每日一次共 21 天) 可抑制 SW837 结直肠癌异种移植模型中表现出强效的抗肿瘤活性[1]。
KRAS G12C-IN-74 (30-100 mg/kg; p.o.; 每日一次共 9-18 天) 在 H1373 肺癌异种移植模型中表现出具有统计学意义但作用温和的单药活性，与 ML385、RBN-2397、PR-619 联合具有协同抗肿瘤活性[1]。

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

Animal Model: NU/NU nude mice (~6 weeks old, 20-25 g)[1]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: p.o.; daily; 21 days
Result: Demonstrated a tumor growth inhibition (TGI) rate of 94.2% at 10 mg/kg.
Achieved complete tumor responses in 2 out of 5 mice at 30 mg/kg.
Maintained stable body weights across all treatment groups throughout the 21-day study.
Animal Model: NU/NU nude mice (~6 weeks old, 20-25 g)[1]
Dosage: 100 mg/kg
Administration: p.o.; daily; 21 days
Result: Achieved a tumor growth inhibition (TGI) rate of 87.2%.
Animal Model: NU/NU nude mice (~6 weeks old, 20-25 g)[1]
Dosage: 30 mg/kg; 100 mg/kg
Administration: p.o.; daily; 18 days
Result: Demonstrated statistically significant tumor growth inhibition at 100 mg/kg, with modest overall therapeutic efficacy compared to activity in other models.
Animal Model: NU/NU nude mice (~6 weeks old, 20-25 g)[1]
Dosage: 100 mg/kg (in combination with 25 mg/kg ML385)
Administration: p.o.; daily; 9 days (KRAS G12C-IN-74); i.p.; daily; 9 days (ML385)
Result: Produced substantially enhanced antitumor efficacy when combined with 25 mg/kg ML385, with significantly greater tumor growth inhibition than either monotherapy.
Animal Model: NU/NU nude mice (~6 weeks old, 20-25 g)[1]
Dosage: 30 mg/kg (in combination with 10 mg/kg RBN-2397)
Administration: p.o.; daily; 15 days
Result: Displayed marked synergistic tumor growth inhibition when combined with 10 mg/kg RBN-2397, overcoming H1373 resistance to single-agent KRAS G12C inhibition.
Animal Model: NU/NU nude mice (~6 weeks old, 20-25 g)[1]
Dosage: 30 mg/kg (in combination with 5 mg/kg PR-619); 100 mg/kg (in combination with 5 mg/kg PR-619)
Administration: p.o.; daily; 15 days (KRAS G12C-IN-74); i.p.; every other day; 7 days (PR-619)
Result: Achieved a tumor growth inhibition (TGI) rate of 50.6% when 30 mg/kg was combined with 5 mg/kg PR-619.
Achieved a TGI rate of 66.3% when 100 mg/kg was combined with 5 mg/kg PR-619, with 1 out of 4 mice showing complete tumor remission.
Did not show statistically significant activity versus control as a single agent at 30 mg/kg.
分子量

615.76

Formula

C33H38FN7O2S
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-74 相关分类

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  • 稀释计算器

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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-743085516-79-3RasApoptosiscolorectal cancer xenograft modelslung cancer xenograft modelsKRAS G12CapoptosisGDP-bound conformationCys12G0/G1 cell cycle arrestpancreatic cancer xenograft modelsKRAS G12C-mutant cancer cellsNCI-H358Inhibitorinhibitorinhibit

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