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Adagrasib

Adagrasib structure

CAS No:
2326521-71-3
Formula:
C32H35ClFN7O2
Chemical Name:
Adagrasib
Synonyms:
MRTX849;MRTX-849;MRTX 849;2-PIPERAZINEACETONITRILE, 4-[7-(8-CHLORO-1-NAPHTHALENYL)-5,6,7,8-TETRAHYDRO-2-[[(2S)-1-METHYL-2-PYRR;2-Piperazineacetonitrile, 4-[7-(8-chloro-1-naphthalenyl)-5,6,7,8-tetrahydro-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]pyrido[3,4-d]pyrimidin-4-yl]-1-(2-fluoro-1-oxo-2-propen-1-yl)-, (2S)-;2-[(2S)-4-[7-(8-chloronaphthalen-1-yl)-2-[[(2S)-1-methylpyrrolidin-2-yl]methoxy]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]-1-(2-fluoroprop-2-enoyl)piperazin-2-yl]acetonitrile;MRTX849(Adagrasib);Adagrasib/MRTX-849;Adagrasib;4-[7-(8-CHLORO-1-NAPHTHALENYL)-5,6,7,8-TETRAHYDRO-2-[[(2S)-1-METHYL-2-PYRR
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

KRAS G12C Inhibitor MRTX849 is an orally available, small molecule inhibitor that targets the oncogenic KRAS substitution mutation, G12C, with potential antineoplastic activity. Upon oral administration MRTX849 covalently binds to cytosine 12 within the switch II pocket of GDP-bound KRAS G12C, thereby inhibiting mutant KRAS-dependent signaling. KRAS, a member of the RAS family of oncogenes, serves an important role in cell signaling, division and differentiation. Mutations of KRAS may induce constitutive signal transduction leading to tumor cell growth, proliferation, invasion, and metastasis.

MRTX-849 was identified as a potent, selective, and covalent KRASG12C inhibitor that exhibits favourable drug-like properties, modifies mutant cysteine 12 in GDP-bound KRASG12C, and inhibits KRAS-dependent signalling. MRTX-849 demonstrated pronounced tumour regression in 17 of 26 (65%) KRASG12C-positive cell line- and patient-derived xenograft models from multiple tumour types, and objective responses have been observed in patients with KRASG12C-positive lung and colon adenocarcinomas[1].

Adagrasib is an orally available, potent, irreversible, small molecule inhibitor of KRAS G12C mutant isoform being developed by Mirati Therapeutics for the treatment of solid tumours harbouring KRAS G12C oncogenic driver mutation, including non-small cell lung cancer (NSCLC) and colorectal cancer (CRC).

Class: non-kinase; Treatment: KRAS(G12C) NSCLC; Other name: MRTX849; Elimination half-life: 24 h; Protein binding = 98.3%

Adagrasib Basic Attributes

Molecular Weight：

604.12

Exact Mass：

603.2524792

UNII：

8EOO6HQF8Y

NCI Thesaurus Code：

C157493

Color/Form：

White to yellow

Characteristics

Density：

1.295±0.06 g/cm3(Predicted)

Boiling Point：

860.2±75.0 °C(Predicted)

PKA：

9.31±0.40(Predicted)

Critical Temperature & Pressure：

Store at -20°C

Safety Information

Storage features：

Store at -20°C

Drug Information

MeSH：

Substances that inhibit or prevent the proliferation of NEOPLASMS. (See all compounds classified as Antineoplastic Agents.)

MeSH Entry Terms：

2-((S)-4-(7-(8-chloronaphthalen-1-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido(3,4-d)pyrimidin-4-yl)-1-(2-fluoroacryloyl)piperazin-2-yl)acetonitrile

Adagrasib Use and Manufacturing

MRTX 849 is used as combination therapy for treatment of cancer.

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