| Identification | Back Directory | [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 | [CAS]
2206736-04-9 | [Synonyms]
MRTX-1257
2-((S)-1-ACRYLOYL-4-(7-(8-METHYLNAPHTHALEN-1-YL)-2-(((S)-1-METHYLPYRROLIDIN-2-YL)METHOXY)-5,6,7,8-TE
2-((2S)-1-acryloyl-4-(7-(8-methylnaphthalen-1-yl)-2-((1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)piperazin-2-yl)acetonitrile
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
2-[(2S)-4-[7-(8-methylnaphthalen-1-yl)-2-[[(2S)-1-methylpyrrolidin-2-yl]methoxy]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]-1-prop-2-enoylpiperazin-2-yl]acetonitrile
2-Piperazineacetonitrile, 1-(1-oxo-2-propen-1-yl)-4-[5,6,7,8-tetrahydro-7-(8-methyl-1-naphthalenyl)-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]pyrido[3,4-d]pyrimidin-4-yl]-, (2S)- | [Molecular Formula]
C33H39N7O2 | [MDL Number]
MFCD31813777 | [MOL File]
2206736-04-9.mol | [Molecular Weight]
565.71 |
| Chemical Properties | Back Directory | [Boiling point ]
845.5±75.0 °C(Predicted) | [density ]
1?+-.0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C, stored under nitrogen | [solubility ]
DMSO : 55 mg/mL (97.22 mM; Need ultrasonic) | [form ]
A crystalline solid | [pka]
9.31±0.40(Predicted) | [color ]
Off-white to pink |
| Hazard Information | Back Directory | [Uses]
MRTX-1257 is irreversible inhibitor of KRAS G12C. Combination therapies comprising KRAS G12C inhibitors and CDK 4/6 inhibitors for treating KRAS G12C cancers. | [in vivo]
MRTX-1257 (1 mg/kg、3 mg/kg、10 mg/kg、30 mg/kg 和 100 mg/kg，每天口服，持续 30 天) 在 MIA PaCa-2 的所有剂量组中均显示出快速的肿瘤生长抑制小鼠 G12C 异种移植模型[1]。
MRTX-1257 在 3、10、30 和 100 mg/kg 剂量组显示持续消退[1]。
每天 100 mg/kg 的 MRTX-1257 导致完全反应，在停止处理后维持 >70 天[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.
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| [IC 50]
KRAS(G12C) |
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