MRTX-849

ChemicalBook > CAS DataBase List > MRTX-849

Product Name: MRTX-849
CAS No.: 2326521-71-3
Chemical Name: MRTX-849
Synonyms: Adagrasib;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;MRTX-849;MTRX-849;Adagrasib/MRTX-849;MRTX849(Adagrasib);Azvudine Impurity 23;MRTX849;MRTX-849;MRTX 849;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-PYRR
CBNumber: CB94918285
Molecular Formula: C32H35ClFN7O2
Formula Weight: 604.12
MOL File: 2326521-71-3.mol

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MRTX-849 Property

Boiling point:: 860.2±75.0 °C(Predicted)
Density: 1.295±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: Soluble in DMSO:1.0(Max Conc. mg/mL);1.7(Max Conc. mM)
form: A crystalline solid
pka: 9.31±0.40(Predicted)
color: White to yellow
InChIKey: PEMUGDMSUDYLHU-ZEQRLZLVSA-N
SMILES: N1(C(=O)C(F)=C)CCN(C2N=C(OC[C@@H]3CCCN3C)N=C3CN(C4=C5C(C=CC=C5Cl)=CC=C4)CCC3=2)C[C@@H]1CC#N

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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-0105265
Product name: MRTX849
Purity: 99.72%
Packaging: 10mg
Price: $115
Updated: 2021/12/16

ChemScene

Product number: CS-0105265
Product name: MRTX849
Purity: 99.72%
Packaging: 25mg
Price: $250
Updated: 2021/12/16

ChemScene

Product number: CS-0105265
Product name: MRTX849
Purity: 99.72%
Packaging: 50mg
Price: $450
Updated: 2021/12/16

ChemScene

Product number: CS-0105265
Product name: MRTX849
Purity: 99.72%
Packaging: 100mg
Price: $680
Updated: 2021/12/16

ChemScene

Product number: CS-0105265
Product name: MRTX849
Purity: 99.72%
Packaging: 500mg
Price: $2150
Updated: 2021/12/16

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MRTX-849 Chemical Properties,Usage,Production

Description

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].

Uses

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

brand name

Krazati

General Description

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

Biological Activity

To minimize GSH metabolism, the development candidate MRTX-849 employed a 2-fluoroacrylamide warhead, imparting whole blood stability of >50 h t1/2 across species while maintaining tractable cellular potency (IC50 = 5–14 nM). Metabolism studies of MRTX-849 in hepatocytes showed that GSH conjugation of the 2-fluoroacrylamide was reduced compared to previous analogues containing the unsubstituted acrylamide. Favorable in vitro ADME and physical properties of MRTX-849 translated into moderate to high bioavailability of 26–63% across species tested. In a PK/PD experiment dosed at 10, 30, and 100 mg/kg to NCI-H358 tumor-bearing mice, MRTX-849 demonstrated dose-dependent protein modification with nearly maximal effect at the highest doses[2].

Mechanism of action

Adagrasib selectively modified mutant cysteine 12 in GDP-bound G12C and inhibited KRASdependent signaling.

Clinical Use

Adagrasib is an irreversible inhibitor of the RAS GTPase family. It is approved by the FDA for the treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) who have been identified by testing as having a KRAS (G12C) mutation.

target

Primary target: KRAS(G12C)

storage

Store at -20°C

References

[1] Jay B. Fell. “Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer.” Journal of Medicinal Chemistry 63 13 (2020): 6679–6693.
[2] J. Christensen. “The KRASG12C Inhibitor, MRTX849, Provides Insight Toward Therapeutic Susceptibility of KRAS Mutant Cancers in Mouse Models and Patients.” Cancer discovery (2019).

MRTX-849 Preparation Products And Raw materials

Raw materials

Preparation Products

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MRTX-849 Suppliers

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View Lastest Price from MRTX-849 manufacturers

BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.

Product: Adagrasib 2326521-71-3
Price: US $0.00/g
Min. Order: 1g
Purity: More Than 99%
Supply Ability: 100kg/Month
Release date: 2024-07-18

Zhengzhou Anbu Chem Co.,Ltd

Product: MRTX-849 2326521-71-3
Price: US $0.00/KG
Min. Order: 0.1KG
Purity: 98%
Supply Ability: 1000KGS
Release date: 2023-07-14

Anhui Zhongda Biotechnology Co., Ltd

Product: MRTX-849 2326521-71-3
Price: US $0.00-0.00/g
Min. Order: 1g
Purity: 99%
Supply Ability: 100000tons
Release date: 2023-08-10

2326521-71-3, MRTX-849Related Search:

MRTX0902 MRTX1133 MRTX-1719 INDEX NAME NOT YET ASSIGNED MRTX-EX185

MRTX-849

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-((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

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

inhibit,GDP-bound,mutant,MIA PaCa-2,MRTX-849,Adagrasib,selective,Inhibitor,MRTX 849,inactive,state,G12C,H1373,covalent,anti-tumor,KRAS,Ras,cells

2-PIPERAZINEACETONITRILE,4-[7-(8-CHLORO-1-NAPHTHALENYL)-5,Chemicalbook6,7,8-TETRAHYDRO-2-[[(2S)-1-METHYL-2-PYRR

2-[(S)-4-[7-(8-chloro-1-naphthyl)-2-[[(S)-1-methyl-2-pyrrolidinyl]methoxy]-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl]-1-(2-fluoroacryloyl)-2-piperazinyl]acetonitrile

MTRX-849

Azvudine Impurity 23

2326521-71-3

api

2326521-71-3