2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. KRAS G12C-IN-75

KRAS G12C-IN-75 是一种口服有效且可穿透血脑屏障的 KRASG12C 抑制剂，其 IC50 为 0.53 nM。KRAS G12C-IN-75 可减弱 P-糖蛋白 (P-gp) 和乳腺癌耐药蛋白 (BCRP) 介导的主动转运。KRAS G12C-IN-75 可抑制肿瘤生长，调控下游 MAPK 靶基因 DUSP6 和 SPRY4 的表达，并在 KRASG12C 阳性异种移植模型中呈现剂量依赖性的 KRASG12C 烷基化作用。KRAS G12C-IN-75 可用于非小细胞肺癌的相关研究。

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KRAS G12C-IN-75

KRAS G12C-IN-75 Chemical Structure

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KRAS G12C-IN-75 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-75 is an orally active, blood-brain barrier penetrant KRASG12C inhibitor with an IC50 of 0.53 nM. KRAS G12C-IN-75 attenuates active transport mediated by P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP). KRAS G12C-IN-75 inhibits tumor growth, regulates the expression of downstream MAPK target genes DUSP6 and SPRY4, and exhibits dose-dependent KRASG12C alkylation in KRASG12C-positive xenograft models. KRAS G12C-IN-75 can be used for research related to non-small cell lung cancer[1].

IC50 & Target[1]

KRas G12C

0.53 nM (IC50)

体外研究
(In Vitro)

KRAS G12C-IN-75 (compound 15) (18 h) 可抑制 HCC1171 细胞中 KRASG12C 的烷基化，其 IC50 为 17 nM[1]。
KRAS G12C-IN-75 (1 μM; 180 min) 在工程化 gMDCK 细胞中的 MDR1 外排率为 4，BCRP 外排率为 3[1]。

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

KRAS G12C-IN-75 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route CLplasma Vdss T1/2 AUC0-∞ Bioavailability
Mice[1] 2 mg/kg i.v. 7 mL/min/kg 0.97 L/kg 1.9 h / /
Mice[1] 6 mg/kg p.o. / / / 5.2 nM·h 20 %
Mice[1] 2 mg/kg i.v. 22 mL/min/kg 2.5 L/kg 2.5 h / /
Mice[1] 6 mg/kg p.o. / / / 3.6 μM·h 43 %
Mice[1] 1 mg/kg i.v. 17 mL/min/kg 5.4 L/kg 6.3 h / /
Mice[1] 2 mg/kg p.o. / / / 3.1 μM·h 83 %
体内研究
(In Vivo)

KRAS G12C-IN-75 (compound 15) (1-30 mg/kg；口服；每日一次；连续 21 天) 可在 NCI-H358 异种移植模型中诱导剂量依赖性抗肿瘤活性[1]。
KRAS G12C-IN-75 (10-200 mg/kg；口服；每日一次；连续 21 天) 可在 NCI-H2122 异种移植模型中诱导剂量依赖性抗肿瘤活性[1]。
KRAS G12C-IN-75 (10-30 mg/kg；口服；单次给药) 可在 NCI-H358 异种移植瘤中结合 KRASG12C 并以剂量依赖方式抑制 MAPK 通路信号传导，在单次口服给药后 8-16 小时达到最大活性[1]。
KRAS G12C-IN-75 (30-100 mg/kg；口服；单次给药) 可剂量依赖性地结合 KRASG12C 并抑制 NCI-H2122 异种移植瘤中的 MAPK 通路信号传导，需采用 100 mg/kg 的剂量才能在单次灌胃给药后 8 小时实现 >90%的靶点烷基化[1]。

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

Animal Model: C.B-17 SCID (inbred, female)[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: p.o.; daily; 21 days
Result: Reduced tumor growth relative to vehicle control at 1 mg/kg.
Achieved tumor stasis at 3 mg/kg.
Induced deep tumor volume regressions at 10 mg/kg and 30 mg/kg.
Caused no loss of body weight in treated mice.
Animal Model: nu/nu (nude, female)[1]
Dosage: 10 mg/kg; 30 mg/kg; 100 mg/kg; 200 mg/kg
Administration: p.o.; daily; 21 days
Result: Reduced tumor growth relative to vehicle control at 10 mg/kg.
Achieved tumor stasis at 30 mg/kg and 100 mg/kg.
Observed a reduction in tumor size over the 21-day study at 200 mg/kg.
Caused no loss of body weight in treated mice.
Animal Model: C.B-17 SCID (inbred, female; tumors grown to 300-500 mm3)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: p.o.; single dose
Result: Observed dose-dependent alkylation of KRAS G12C and reduction in mRNA expression of downstream MAPK target genes DUSP6 and SPRY4 at 10 mg/kg, with maximal target engagement and pathway inhibition at 8-16 hours post-dose, followed by gradual rebound over 72 hours.
Induced greater magnitude and duration of KRAS G12C alkylation (> 90% reduction in unalkylated KRAS G12C at 8 hours) and pathway inhibition at 30 mg/kg, with maximal effects at 8-16 hours post-dose.
Animal Model: nu/nu (nude, female; tumors grown to 300-500 mm3)[1]
Dosage: 30 mg/kg; 100 mg/kg
Administration: p.o.; single dose
Result: Observed partial alkylation of KRAS G12C and reduction in DUSP6 and SPRY4 mRNA expression at 30 mg/kg.
Achieved > 90% alkylation of KRAS G12C at 8 hours post-dose, with corresponding robust reduction in DUSP6 and SPRY4 mRNA expression, correlating directly with target engagement at 100 mg/kg.
分子量

538.90

Formula

C25H20ClF5N4O2
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-75 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-75RasMAPK pathwayP-glycoprotein (P-gp)CD-1 miceGDP-bound statebreast cancer resistance protein (BCRP)Cys12Sprague-Dawley ratsSPRY4KRAS G12CDUSP6Inhibitorinhibitorinhibit

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