MRTX1257
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MedKoo CAT#: 207086

CAS#: 2206736-04-9

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.


Chemical Structure

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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
5.0mg USD 150.0 Ready to ship
10.0mg USD 250.0 Ready to ship
25.0mg USD 450.0 Ready to ship
50.0mg USD 750.0 Ready to ship
100.0mg USD 1250.0 Ready to ship
200.0mg USD 1950.0 Ready to ship
500.0mg USD 3150.0 Ready to ship
1.0g USD 4950.0 Ready to ship
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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

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 55.0 97.2

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

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https://www.mirati.com/wp-content/uploads/2018/12/KRAS-Poster-AACR-RAS.pdf