2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. KRAS G12D inhibitor 22

KRAS G12D inhibitor 22 (compound 6) 是一种 KRAS 突变抑制剂。KRAS G12D inhibitor 22 抗肿瘤活性高 (IC50<100 nM)，选择性好，毒性低。KRAS G12D inhibitor 22 可用于乳腺癌研究。

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KRAS G12D inhibitor 22

KRAS G12D inhibitor 22 Chemical Structure

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KRAS G12D inhibitor 22 相关抗体

Top Publications Citing Use of Products

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K-Ras H-Ras N-Ras Ras

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KRAS G12D inhibitor 22 (compound 6) is a inhibitor of KRAS mutation. KRAS G12D inhibitor 22 has high activity (IC50＜100 nM), good selectivity and low toxicity.KRAS G12D inhibitor 22 can be used in breast cancer research[1].

IC50 & Target[1]

KRas G12D

<100 nM (IC50)

体外研究
(In Vitro)

KRAS G12D inhibitor 22 (0.08-20 μM; 72 h) 对 AGS 细胞生长有良好的抑制作用 (IC50＜500 nM)[1]。
KRAS G12D inhibitor 22 对 KRAS G12D 蛋白有较高的抑制作用 (IC50<100 nM)[1]。
KRAS G12D inhibitor 22 (0.08-20 μM; 72 h) 对 ASPC-1 和 AGS 细胞的抗增殖活性优于 MRTX1133 (HY-134813)，对其他 Kras G12C 突变细胞系具有更好的选择作用[1]。

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

KRAS G12D inhibitor 22 相关抗体:

Cell Proliferation Assay[1]

Cell Line: AGS, AsPC-K, NCI-H358, MOLM13 cells
Concentration: 0.08-20 μM
Incubation Time: 72 h
Result: Had good inhibitory effect on the growth of Kras, Gl2D mutant AGS, ASPC-1 cells.
Had weak inhibitory effect on the growth of KRASG12C-mutated cell line NCI-H358 and Kras wild-type cell line MOLMl3.
体内研究
(In Vivo)

KRAS G12D inhibitor 22 (3，5 mg/kg；i.v. 和 i.p.；0-24 h) 单次给药后能够达到抑制肿瘤细胞生长的药物起效浓度，且具有较好的生物利用度在 SD 大鼠体内[1]。
Pharmacokinetic Analysis in Male SD ratl[1]

Route Dose (mg/kg) T1/2 (h) Cmax (ng/mL) Tmax (h) CL (mL/min/kg) Vss (L/kg) AUG0_t (ng/mL h) 生物利用度 (%)
i.v. 5 0.63 2163 0.08 96.4 3.5 1128 /
i.p. 3 1.03 177 0.25 / / 255.8 37.79

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

Animal Model: Male SD rat[1]
Dosage: 3 and 5 mg/kg
Administration: i.v. and i.p.
Result: Reached the effective concentration of inhibiting tumor cell growth after a single administration, and has good bioavailability.
分子量

644.66

Formula

C35H32F4N6O2
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 G12D inhibitor 22 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

KRAS G12D inhibitor 22RasASPC-1 cellsKRAS G12Dpancreatic cancerInhibitorinhibitorinhibit

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目录号：
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