Welcome to ProbeChem!Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : MRTX-EX185
CAS No.: 2621927-57-7
Catalog No.: PC-38438Not For Human Use, Lab Use Only.
MRTX-EX185 (EX185) is a novel potent small-molecule inhibitor of KRAS mutants, exhibits target engagement against KRAS (G12D) with IC50 of 90 nM, binds to GDP-loaded KRAS and KRAS(G12D), as well as the active GNP state.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $358 | In stock | |
| 10 mg | $558 | In stock | |
| 25 mg | $898 | 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-EX185 (EX185) is a novel potent small-molecule inhibitor of KRAS mutants, exhibits target engagement against KRAS (G12D) with IC50 of 90 nM, binds to GDP-loaded KRAS and KRAS(G12D), as well as the active GNP state.
MRTX-EX185 also bound GDP-loaded HRAS.
MRTX-EX185 engages both nucleotide states-albeit with preference for the inactive GDP-loaded protein-and might present an opportunity to inhibit even constitutively active (GTP-loaded) KRAS hotspot mutants
MRTX-EX185 engages numerous KRAS Q61, G12 and G13 mutant proteins and drives antiproliferation.
| M.Wt | 564.665 | |
| Formula | C33H33FN6O2 | |
| Appearance | Solid | |
| Storage |
|
|
| Solubility |
10 mM in DMSO |
|
| Chemical Name/SMILES |
4-[4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-ylmethoxy)pyrido[4,3-d]pyrimidin-7-yl]-5-ethynylnaphthalen-2-ol |
|
1. James D Vasta, et al. Nat Chem Biol. 2022 Mar 21. doi: 10.1038/s41589-022-00985-w.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
