WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 207086
Description: MRTX1257 is a potent, selective, covalent and irreversible inhibitor of KRAS G12C. MRTX1257 inhibited KRAS dependent ERK phosphorylation in the H358cell assay with an IC50= 900 pM. MRTX1257 demonstrated 31% bioavailability in the mouse, with free fraction exposures well above the cellular potency. In a PK/PD experiment, 77% target engagement.
MedKoo Cat#: 207086
Chemical Formula: C33H39N7O2
Exact Mass: 565.3165
Molecular Weight: 565.72
Elemental Analysis: C, 70.06; H, 6.95; N, 17.33; O, 5.66
Synonym: MRTX1257; MRTX-1257; MRTX 1257;
IUPAC/Chemical Name: 2-((S)-1-acryloyl-4-(7-(8-methylnaphthalen-1-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)piperazin-2-yl)acetonitrile
InChi Key: YRYQLVCTQFBRLD-UIOOFZCWSA-N
InChi Code: InChI=1S/C33H39N7O2/c1-4-30(41)40-19-18-39(20-25(40)13-15-34)32-27-14-17-38(29-12-6-10-24-9-5-8-23(2)31(24)29)21-28(27)35-33(36-32)42-22-26-11-7-16-37(26)3/h4-6,8-10,12,25-26H,1,7,11,13-14,16-22H2,2-3H3/t25-,26-/m0/s1
SMILES Code: N#CC[C@@H]1N(C(C=C)=O)CCN(C2=C3C(CN(C4=C5C(C)=CC=CC5=CC=C4)CC3)=NC(OC[C@H]6N(C)CCC6)=N2)C1
Appearance: Solid powder
Purity: >95% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
|Biological target:||MRTX-1257 is a covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells.|
|In vitro activity:||TBD|
|In vivo activity:||TBD|
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 565.72 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
|In vitro protocol:||TBD|
|In vivo protocol:||TBD|