For research use only. Not for therapeutic Use.
MRTX-EX185 formic is a potent inhibitor of GDP-loaded KRAS and KRAS(G12D), with an IC50 of 90 nM for KRAS(G12D). MRTX-EX185 formic also binds GDP-loaded HRAS[1]. MRTX-EX185 (formic) is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
| Catalog Number | I043568 |
| Synonyms | 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;formic acid |
| Molecular Formula | C34H35FN6O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C33H33FN6O2.CH2O2/c1-2-20-6-3-7-21-14-24(41)15-25(27(20)21)29-28(34)30-26(16-35-29)31(39-17-22-8-9-23(18-39)36-22)38-32(37-30)42-19-33-10-4-12-40(33)13-5-11-33;2-1-3/h1,3,6-7,14-16,22-23,36,41H,4-5,8-13,17-19H2;1H,(H,2,3)/t22-,23+; |
| InChIKey | YWOAMEBABPMBDA-ZJXXCOCUSA-N |
| SMILES | C#CC1=CC=CC2=CC(=CC(=C21)C3=NC=C4C(=C3F)N=C(N=C4N5CC6CCC(C5)N6)OCC78CCCN7CCC8)O.C(=O)O |
| Reference | [1]. Vasta JD, et, al. KRAS is vulnerable to reversible switch-II pocket engagement in cells. Nat Chem Biol. 2022 Mar 21. |
