计算溶液所需的质量、体积或浓度。
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 1 篇同行评审文献引用。
概述
MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated K D against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations
In Vitro
MRTX1133 inhibits ERK phosphorylation in the AGS cell line with an IC 50 ranging 1-10 nM (AsPC-1, Panc 04.03, Panc 02.03, SW1990, GP2D, Suit2, A427, SNU1033, and HPAC cells). In a 2D viability assay, the IC 50 of MRTX1133 is 6 nM against AGS cells (KRAS G12D), while demonstrating more than 500-fold selectivity against MKN1, a cell line which is dependent on KRAS for its growth and survival due to the amplification of wild-type KRAS. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MRTX1133 displays efficacious in a KRAS G12D mutant xenograft mouse tumor model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-8-weekold, female, athymic nude-Foxn1 nu mice (Panc 04.03 model) Dosage: 3, 10, or 30 mg/kg Administration: Intraperitoneal; twice a day for 28 days Result: An antitumor efficacy study in this model resulted in MRTX1133 dose-dependent antitumor activity with 94% growth inhibition observed at 3 mg/kg BID (IP) and tumor regressions of -62% and -73% observed at 10 and 30 mg/kg BID (IP), respectively.
IC50& Target:KRas G12D 0.2 pM (Kd)
规格
规格或纯度
Moligand™, 10mM in DMSO
英文名称
MRTX1133
生化机理
MRTX1133 是一种非共价、强效和选择性的 KRAS G12D 抑制剂。MRTX1133 能以最佳方式填充开关 II 口袋，并扩展三个取代基，从而与蛋白质产生有利的相互作用，因此对 KRAS G12D 的 K D 值估计为 0.2 pM。MRTX1133
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C#CC1=C(C=CC2=CC(=CC(=C21)C3=NC=C4C(=C3F)N=C(N=C4N5CC6CCC(C5)N6)OC[C@@]78CCCN7C[C@@H](C8)F)O)F
PubChem CID
分子量
600.63
技术文档
高级数据
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
2025 KRAS靶向药物进展
目录： 技术文章
此产品的引用文献
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