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MedKoo Cat#: 207086 | Name: MRTX1257
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

MRTX1257
MRTX1257
CAS#2206736-04-9

Theoretical Analysis

MedKoo Cat#: 207086

Name: MRTX1257

CAS#: 2206736-04-9

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

Price and Availability

Size Price Availability Quantity
5mg USD 150.00 Ready to ship
10mg USD 250.00 Ready to ship
25mg USD 450.00 Ready to ship
50mg USD 750.00 Ready to ship
100mg USD 1,250.00 Ready to ship
200mg USD 1,950.00 Ready to ship
500mg USD 3,150.00 Ready to ship
1g USD 4,950.00 Ready to ship
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Related CAS #
No Data
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
More Info
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 mg/mL mM
Solubility
DMSO 55.0 97.20
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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
Formulation protocol:
TBD
In vitro protocol:
TBD
In vivo protocol:
TBD
Laurent PA, Milic M, Quevrin C, Meziani L, Liu W, Morel D, Signolle N, Clémenson C, Levy A, Mondini M, Deutsch E. KRASG12C inhibition using MRTX1257: a novel radio-sensitizing partner. J Transl Med. 2023 Oct 31;21(1):773. doi: 10.1186/s12967-023-04619-0. PMID: 37907934; PMCID: PMC10619254.