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| | 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 Basic information |
| Product 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: | 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;MRTX-1257;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-TE;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)-;Inhibitor,MRTX 1257,selective,inhibit,Ras,G12C,irreversible,MRTX1257,ERK,phosphorylation,MRTX-1257,H358 cells,cancer,mutant,covalent,KRAS;MRTX1257 (MRTX-1257) | | CAS: | 2206736-04-9 | | MF: | C33H39N7O2 | | MW: | 565.71 | | EINECS: | | | Product Categories: | methylnaphthale;APIs | | Mol File: | 2206736-04-9.mol | ![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 Structure](CAS/20200331/GIF/2206736-04-9.gif) |
| | 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 Chemical Properties |
| 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 |
| | 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 Usage And Synthesis |
| 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, and 100 mg/kg, orally daily for 30 days) demonstrated rapid tumor growth inhibition in all dose groups in the MIA PaCa-2 mouse G12C xenograft model[1].
MRTX-1257 demonstrated sustained regressions in the 3, 10, 30, and 100 mg/kg dose groups[1].
MRTX-1257 at 100 mg/kg daily resulted in complete responses that were maintained for >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. |
| | IC 50 | KRAS(G12C) |
| | 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 Preparation Products And Raw materials |
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