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

KRASG12C IN-2 (化合物 17) 是一种口服有效的 KRASG12C 抑制剂。KRASG12C IN-2 能有效抑制小鼠体内肿瘤生长。

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KRASG12C IN-2 Chemical Structure

KRASG12C IN-2 Chemical Structure

CAS No. : 2706637-12-7

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KRASG12C IN-2 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-2 (compound 17) is an orally active KRASG12C inhibitor. KRASG12C IN-2 inhibits tumor growth in mice[1].

IC50 & Target

KRASG12C[1].
体外研究
(In Vitro)

KRASG12C IN-2 (0-100 nM;72 h) 抑制 MIA-PA-CA-2细胞 (KRASG12C 突变) 增殖，IC50 值为 0.44 nM[1]。

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

KRASG12C IN-2 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MIA-PA-CA-2 cells (with KRASG12C mutant)
Concentration: 0-100 nM
Incubation Time: 72 h
Result: Exhibited antiproliferation activity (IC50 = 0.44 nM).
体内研究
(In Vivo)

KRASG12C IN-2 (10, 30 mg/kg; p.o.; single daily for 22 days) 抑制小鼠体内肿瘤生长[1]。

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

Animal Model: Nude Balb/c mice (Subcutaneous transplantation model of Mia PaCa-2 cells)[1].
Dosage: 10, 30 mg/kg
Administration: Oral administration; single daily for 22 days.
Result: Inhibited tumor growth in mice, and the inhibition rates are 93.06% (dosage at 10 mg/kg) and 99.64% (dosage at 30 mg/kg), respectively.
Animal Model: Male SD rats and male CD mice[1].
Dosage: 2.0 mg/kg
Administration: i.v.; single
Result: 1.19 Pharmacokinetic Parameters of KRASG12C IN-2 in Male SD rats and Male CD mice[1].
Male SD rats Male CD mice
IV (2 mg/kg) IV (2 mg/kg)
T1/2 (h) 1.9 1.7
CL (mL/min/kg) 71.5 40.6
Vdss/Vdss, u(L/kg) 10.6/221 3.9/32.3
AUC0-last/AUCu (nM•h) 653/31.3 1297/155.6
Animal Model: Male SD rats and male CD mice[1].
Dosage: 9.8, 10.3 mg/kg
Administration: p.o.; single
Result: 1.19 Pharmacokinetic Parameters of KRASG12C IN-2 in Male SD rats and Male CD mice[1].
Male SD rats Male CD mice
PO (9.8 mg/kg) PO (10.3 mg/kg)
AUC0-last/AUCu (nM•h) 995/47.8 1422/170.6
Tmax (h) 1.5 1.0
Cmax/Cmax, u (nM) 220/10.6 431/51.7
F (%) 30.5% 21.9%
分子量

679.66

Formula

C32H35F6N7O3
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-2 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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-22706637-12-7RasMIA-PA-CA-2 cellscancerInhibitorinhibitorinhibit

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目录号：
HY-153262
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