Welcome to Shanghai Probechem Biochemicals Co Ltd !Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : MRTX1133
CAS No.: 2621928-55-8
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $248 | In stock | |
| 10 mg | $378 | In stock | |
| 25 mg | $588 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
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.
| M.Wt | 600.646 | |
| Formula | C33H31F3N6O2 | |
| Appearance | Solid | |
| Storage |
|
|
| 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- |
|
1. Xiaolun Wang, et al. J Med Chem. 2022 Feb 24;65(4):3123-3133.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
