MRTX1133|2621928-55-8|-陌孚医药/Medlife

您当前的位置：

MRTX1133

目录号: PL10878 纯度: ≥99%

CAS No. :2621928-55-8

商品编号	规格	价格	会员价
PL10878-5mg	5mg	¥8197.00	请登录
PL10878-10mg	10mg	¥12536.00	请登录
PL10878-25mg	25mg	¥22501.00	请登录
PL10878-50mg	50mg	询价	询价
PL10878-100mg	100mg	询价	询价
PL10878-10mM*1mLinDMSO	10mM*1mLinDMSO	¥9016.00	请登录

Medlife所售产品仅用于科学研究（非临床研究），非药品不可食用，不可用于人体或动物的临床诊断和治疗，我们不为个人提供产品及服务。产品COA等资料，可至下方“质量控制”中下载。

加入购物车在线咨询收藏产品大包装询价

中文名称	MRTX1133
英文名称	MRTX1133
英文别名	MRTX1133;4-[4-(3,8-diazabicyclo[3.2.1]octan-3-yl)-8-fluoro-2-[[(2R,8S)-2-fluoro-1,2,3,5,6,7-hexahydropyrroliz;BDBM50579601;NSC836407;4-[4-(3,8-diazabicyclo[3.2.1]octan-3-yl)-8-fluoro-2-[[(2R,8S)-2-fluoro-1,2,3,5,6,7-hexahydropyrroliz;4-[4-(3,8-diazabicyclo[3.2.1]octan-3-yl)-8-fluoro-2-[[(2R,8S)-2-fluoro-1,2,3,5,6,7-hexahydropyrrolizin-8-yl]methoxy]pyrido[4,3-d]pyrimidin-7-yl]-5-ethynyl-6-fluoronaphthalen-2-ol
Cas No.	2621928-55-8
分子式	C₃₃H₃₁F₃N₆O₂
分子量	600.63
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	MRTX1133 是一种非共价、强效和选择性 KRAS G12D 抑制剂。MRTX1133 以最佳方式填充开关 II 口袋，并延伸三个取代基以与蛋白质良好地相互作用，对 KRAS G12D 的 K_D 为 0.2 pM。MRTX1133 阻止 SOS1 催化的核苷酸交换和/或KRAS G12D/GTP/RAF1 复合物的形成，从而抑制突变体 KRAS 依赖性信号转导。MRTX1133 选择性抑制 KRAS G12D 突变体肿瘤细胞，但不抑制 KRAS 野生型细胞。MRTX1133 在细胞实验中具有一位数纳摩尔活性，在含有 KRAS G12D 突变的肿瘤模型中具有显著的体内疗效。
生物活性	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.
性状	Solid
IC50 & Target[1][2]	KRas G12D 0.2 pM (Kd)
体外研究(In Vitro)	MRTX1133 inhibits ERK phosphorylation in the AGS cell line with an IC50 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 IC50 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 . has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	MRTX1133 displays efficacious in a KRAS G12D mutant xenograft mouse tumor model. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-8-weekold, female, athymic nude-Foxn1 mice (Panc 04.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Wang X, et al. Identification of MRTX1133, a Noncovalent, Potent, and Selective KRAS G12D Inhibitor [published online ahead of print, 2021 Dec 10]. J Med Chem. 2021;10.1021/acs.jmedchem.1c01688.

溶解度数据	In Vitro: DMSO : 50 mg/mL (83.25 mM; Need ultrasonic)配制储备液

搜索质检报告(COA)

产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

相关产品

The molarity calculator equation

The dilution calculator equation