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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-MRTX1133
MRTX1133

Chemical Structure : MRTX1133

CAS No.: 2621928-55-8

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MRTX1133 (MRTX-1133)

货号: PC-72331Not For Human Use, Lab Use Only.

MRTX-1133 (MRTX1133) is a potent, selective and noncovalent inhibitor KRAS G12D with SPR Kd of 0.2 nM, AlphaLISA IC50 of 5 nM.

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5 mg ￥2480 In stock
10 mg ￥3780 In stock
25 mg ￥5880 In stock
50 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MRTX-1133 (MRTX1133) is a potent, selective and noncovalent inhibitor KRAS G12D with SPR Kd of 0.2 nM, AlphaLISA IC50 of 5 nM.
MRTX1133 inhibited ERK phosphorylation in the AGS cell line with an IC50 of 2 nM, demonstrated high potency against AGS cell line in a 2D viability assay with IC50 of 6 nM, >500-fold selectivity against MKN1, a cell line which is dependent on wild-typ KRAS.
MRTX1133 modulated KRAS-dependent ERK phosphorylation in the Panc 04.03 xenograft tumor model at 30 mg/kg BID (IP), MRTX1133 exhibted 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, no significant antitumor activity in the non-KRASG12D tumor model MKN1.

物理化学性质&存储条件

分子量 600.646
分子式 C33H31F3N6O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO (6 mg/mL in DMSO)
Chemical Name/SMILES

2-Naphthalenol, 4-[4-(3,8-diazabicyclo[3.2.1]oct-3-yl)-8-fluoro-2-[[(2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl]methoxy]pyrido[4,3-d]pyrimidin-7-yl]-5-ethynyl-6-fluoro-

参考文献

1. Xiaolun Wang, et al. J Med Chem. 2022 Feb 24;65(4):3123-3133.

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