MRTX1257|CAS 2206736-04-9|DC Chemicals

Cas No.:	2206736-04-9
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
Synonyms:	MRTX-1257;MRTX 1257
SMILES:	C(#N)C[C@@H]1CN(C2N=C(OC[C@H]3CCCN3C)N=C3CN(C4=C5C(C=CC=C5C)=CC=C4)CCC3=2)CCN1C(=O)C=C
Formula:	C₃₃H₃₉N₇O₂
M.Wt:	565.722
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[1]. Matthew et al. Structure-Based Drug Discovery of MRTX1257, a Selective, Covalent KRAS G12C Inhibitor with Oral Activity in Animal Models of Cancer.

Description:

MRTX-1257 is a selective, irreversible, covalent and oral active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells[1].

In Vivo:

MRTX-1257 (1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg, orally, daily for 30 days) shows rapid tumor growth inhibition at all dose groups in MIA PaCa-2 G12C Xenograft model in mice[1]. MRTX-1257 shows sustained regression at 3,10, 30, and 100 mg/kg dose groups[1]. MRTX-1257 dosed of 100 mg/kg daily leads to complete responses that are maintained >70 days after cessation of treatment[1]. Animal Model: MIA PaCa-2 G12C Xenograft Model (mouse)[1]. Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg. Administration: Orally daily for 30 days. Result: Showed rapid tumor growth inhibition at all dose groups. Showed sustained regression at 3,10, 30, and 100 mg/kg dose groups. 100 mg/kg daily led to complete responses that are maintained >70 days after cessation of treatment.

MSDS

COA

LOT NO.	DOWNLOAD
2018-0101

2018-0101

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