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

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
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 ，S8831;MRTX1257 (MRTX-1257);MRTX-1257, 10 mM in DMSO;2-((S)-1-ACRYLOYL-4-(7-(8-METHYLNAPHTHALEN-1-YL)-2-(((S)-1-METHYLPYRROLIDIN-2-YL)METHOXY)-5,6,7,8-TE;Inhibitor,MRTX 1257,selective,inhibit,Ras,G12C,irreversible,MRTX1257,ERK,phosphorylation,MRTX-1257,H358 cells,cancer,mutant,covalent,KRAS;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)-
CBNumber: CB64845142
Molecular Formula: C33H39N7O2
Formula Weight: 565.71
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 Property

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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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0085392
Product name: MRTX-1257
Purity: 98.62%
Packaging: 5mg
Price: $160
Updated: 2021/12/16

ChemScene

Product number: CS-0085392
Product name: MRTX-1257
Purity: 98.62%
Packaging: 10mg
Price: $280
Updated: 2021/12/16

DC Chemicals

Product number: DC12651
Product name: MRTX1257
Purity: >98%
Packaging: 100mg
Price: $650
Updated: 2021/12/16

Chemenu

Product number: CM328387
Product name: 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
Purity: 95%+
Packaging: 50mg
Price: $1250
Updated: 2021/12/16

DC Chemicals

Product number: DC12651
Product name: MRTX1257
Purity: >98%
Packaging: 1g
Price: $2200
Updated: 2021/12/16

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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,Usage,Production

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

Raw materials

Preparation Products

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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 Suppliers

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2206736-04-9, 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)acetonitrileRelated Search:

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)

MRTX-1257, 10 mM in DMSO

MRTX-1257 ，S8831

2206736-04-9

C33H39N7O2

methylnaphthale

APIs