1. GPCR/G Protein MAPK/ERK Pathway PI3K/Akt/mTOR Stem Cell/Wnt
  2. Ras Akt Raf ERK
  3. KRAS-IN-58

KRAS-IN-58 是一种 KRAS 抑制剂,对 KRASG12DIC50 为 0.223 μM。KRAS-IN-58 可结合 KRASG12C 和 KRASG12D 蛋白,并下调胰腺癌细胞中磷酸化 Raf1AKTERK 的水平。KRAS-IN-58 可用于胰腺癌的研究。

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KRAS-IN-58

KRAS-IN-58 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KRAS-IN-58 is a KRAS inhibitor with a IC50 of 0.223 μM against KRASG12D. KRAS-IN-58 binds to KRASG12C and KRASG12D proteins, and reduces the levels of phosphorylated Raf1, AKT and ERK in pancreatic cancer cells. KRAS-IN-58 can be used for the research of pancreatic cancer[1].

IC50 & Target[1]

KRas G12D

223 nM (IC50)

体外研究
(In Vitro)

KRAS-IN-58 (24 h) 可抑制 ASPC-1、PANC-1 和 Miapac-2 胰腺癌细胞的活力,其 IC50 值分别为 1.16 μM、6.59 μM 和 6.432 μM[1]
KRAS-IN-58 (24 h) 可抑制 SW1990 胰腺癌细胞的活力,其 IC50 为 1.518 μM;而对 LO2 正常肝细胞 (IC50 = 55.53 μM) 和 HPDE6-C7 正常胰腺上皮细胞 (IC50 = 10.50 μM) 的活性则弱得多,显示出对癌细胞相对非癌细胞的选择性活性[1]
KRAS-IN-58 (1.25-20 μM) 可剂量依赖性地下调 ASPC-1 和 Miapac-2 胰腺癌细胞中 KRAS、pRaf1、pAKT 及 pERK 的水平[1]

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

药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax MRT CL Vss Vz AUC
Mice[1] 2 mg/kg i.v. 4.3 h / / 0.512 h 66 mL/min/kg 2.6 L/kg 26 L/kg 510 ng·h/mL
Mice[1] 10 mg/kg p.o. 6.52 h 0.333 h 1.4 ng/mL 2.82 h / / / /
分子量

451.52

Formula

C21H17N5O3S2

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
  • 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.

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KRAS-IN-58
目录号:
HY-182749
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