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ChemicalBook >  Product Catalog >  Organic Chemistry >  Heterocyclic Compounds >  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-((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

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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
Product Categories:
  • methylnaphthale
  • APIs
Mol File:
2206736-04-9.mol
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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 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
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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 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)acetonitrileSupplier

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