Welcome to Shanghai Probechem Biochemicals Co Ltd !Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : MRTX849
CAS No.: 2326521-71-3
Catalog No.: PC-72227Not For Human Use, Lab Use Only.
MRTX849 (Adagrasib, MRTX-849) is a potent, selective, and covalent KRAS G12C inhibitor, inhibits KRAS-dependent signaling.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $88 | In stock | |
| 25 mg | $158 | In stock | |
| 50 mg | $248 | In stock | |
| 100 mg | Get quote | ||
| 200 mg | Get quote | ||
| 1 g | Get quote |
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
MRTX849 (Adagrasib, MRTX-849) is a potent, selective, and covalent KRAS G12C inhibitor, inhibits KRAS-dependent signaling.
MRTX849 (Adagrasib) binds to, stabilizes and selectively modifies mutant cysteine 12 in GDP-bound KRAS G12C, and inhibits KRAS-dependent signaling.
MRTX849 (Adagrasib) inhibited KRAS-dependent signaling targets including ERK1/2 phosphorylation (Thr202/Tyr204 ERK1; pERK), S6 phosphorylation (RSK-dependent Ser235/236; pS6) and expression of the ERK-regulated DUSP6, each with IC50 values in the single-digit nanomolar range in KRASG12C-mutant H358 lung and MIA PaCa-2 pancreatic cancer cell lines.
MRTX849 (Adagrasib) potently inhibited cell growth in the vast majority of KRASG12C-mutant cell lines with IC50 of 10-973 nM.
MRTX849 (Adagrasib) inhibited KRAS signaling and tumor growth in vivo, demonstrated potent anti-tumor activity in KRASG12C-mutant and non KRASG12C-mutant human tumor xenografts models.
| M.Wt | 604.13 | |
| Formula | C32H35ClFN7O2 | |
| Appearance | Solid | |
| Storage |
|
|
| Solubility |
20 mM in DMSO (12.1 mg/mL) |
|
| Chemical Name/SMILES |
2-((S)-4-(7-(8-Chloronaphthalen-1-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)-1-(2-fluoroacryloyl)piperazin-2-yl)acetonitrile |
|
1. Hallin J, et al. Cancer Discov. 2020 Jan;10(1):54-71.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
