AMG 510

Description Biological Activity Storage In vivo

Product Name: AMG 510
CAS No.: 2252403-56-6
Chemical Name: AMG 510
Synonyms: CPD2809;4-((S)-4-acryloyl-2-methylpiperazin-1-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidin-2(1H)-one;Sotorasib (AMG-510);Sotorasib (racemate);Sotorasib (AMG-510) racemate;Pyrido[2,3-d]pyrimidin-2(1H)-one, 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-4-[(2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-;AMG 510;AMG-510，AMG510;Amg 510 Powder;AMG 510 USP/EP/BP
CBNumber: CB24858719
Molecular Formula: C30H30F2N6O3
Formula Weight: 560.59
MOL File: 2252403-56-6.mol

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AMG 510 Property

Boiling point:: 730.5±70.0 °C(Predicted)
Density: 1.36±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C, stored under nitrogen
solubility: DMSO:75.0(Max Conc. mg/mL);133.78(Max Conc. mM)
Water:33.33(Max Conc. mg/mL);59.45(Max Conc. mM)
Ethanol:8.0(Max Conc. mg/mL);14.27(Max Conc. mM)
pka: 6.52±0.35(Predicted)

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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.

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

Biosynth Carbosynth

Product number: BA172505
Product name: AMG 510
Packaging: 5mg
Price: $105
Updated: 2021/12/16

Biosynth Carbosynth

Product number: BA172505
Product name: AMG 510
Packaging: 10mg
Price: $190
Updated: 2021/12/16

ChemScene

Product number: CS-0091978
Product name: Sotorasib(racemate)
Purity: 98.99%
Packaging: 10mg
Price: $200
Updated: 2021/12/16

AK Scientific

Product number: 0113EN
Product name: CID137278711
Packaging: 10mg
Price: $306
Updated: 2021/12/16

Biosynth Carbosynth

Product number: BA172505
Product name: AMG 510
Packaging: 25mg
Price: $425
Updated: 2021/12/16

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AMG 510 Chemical Properties,Usage,Production

Description

AMG-510 is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. AMG-510 irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. AMG-510 is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors.

Biological Activity

AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity.
AMG-510, also known as also known as Sotorasib, is a potent KRAS G12C covalent inhibitor and the active atropisomer separated by chiral HPLC. AMG-510 selectively targets the KRAS p.G12C mutant, at either the DNA, RNA or protein level, and prevents, through an as of yet not elucidated manner, expression of and/or tumor cell signaling through the KRAS p.G12C mutant. This may inhibit growth in KRAS p.G12C-expressing tumor cells.

Storage

-20°C, stored under nitrogen

In vivo

In immune-competent mice, treatment with AMG 510 resulted in a pro-inflammatory tumour microenvironment and produced durable cures alone as well as in combination with immune-checkpoint inhibitors. Cured mice rejected the growth of isogenic KRASG12D tumours, which suggests adaptive immunity against shared antigens. Reference: Nature. 2019 Nov;575(7781):217-223. https://www.nature.com/articles/s41586-019-1694-1

Uses

AMG-510 is a KRAS G12C inhibitor thus leading to the regression of KRAS G12C tumors as it interrupts protein signaling.

Definition

ChEBI: Sotorasib is a pyridopyrimidine that is pyrido[2,3-d]pyrimidin-2(1H)-one substituted by 4-methyl-2-(propan-2-yl)pyridin-3-yl, (2S)-2-methyl-4-(prop-2-enoyl)piperazin-1-yl, fluoro and 2-fluoro-6-hydroxyphenyl groups at positions 1, 4, 6 and 7, respectively. It is approved for the treatment of patients with non-small cell lung cancer having KRAS(G12C) mutations. It has a role as an antineoplastic agent. It is a member of acrylamides, a N-acylpiperazine, a pyridopyrimidine, a member of monofluorobenzenes, a member of methylpyridines, a tertiary carboxamide, a tertiary amino compound and a member of phenols.

in vitro

It was examined whether AMG510 has an antitumor effect on the CACO-2 (human colorectal cancer) cells into which the KRAS G12C (Kirsten rat sarcoma 2 viral oncogene homolog mutation) gene was introduced. The results showed that there was a clear concentration dependent RPR (relative proliferation ratio) decrease and that AMG 510 selectively inhibited KRAS G12C in colon cancer cells in vitro (Fig. 4A). Reference: Mol Clin Oncol. 2021 Jul;15(1):148.

storage

Store at -20°C

AMG 510 Preparation Products And Raw materials

Raw materials

Preparation Products

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AMG 510 Suppliers

China 138 United States 5 Global 143

Wuhan Biocar Pharmacy Co.，Ltd

Tel: 13343447621
Fax: 027-86589876
Email: linkdevil@foxmail.com
Country: China
ProdList: 62
Advantage: 58

Shanghai tingchong biology science and technology co., ltd

Tel: 18964309092 18964309092
Email: 2769493375@qq.com
Country: China
ProdList: 2635
Advantage: 58

Wuhan Bo Jin Biotechnology Co.,Ltd.

Tel: 18164232327
Email: 2709603029@qq.com
Country: China
ProdList: 291
Advantage: 58

BeiJing Hwrk Chemicals Limted

Tel: 0757-86329057 18501085097
Fax: 010-89508210
Email: sales3.gd@hwrkchemical.com
Country: China
ProdList: 7639
Advantage: 55

Wuhan Sunrise Technology Development Co., Ltd.

Tel: 027-027-83314682 13554138826
Fax: +86 (27) 8331-4682
Email: whsrtech@vip.163.com
Country: China
ProdList: 300
Advantage: 62

Daicel Chiral Technologies (China)CO.,LTD

Tel: 021-50460086-9 15921403865
Fax: +86-21-50462321
Email: han_yajun@dctc.daicel.com
Country: China
ProdList: 6854
Advantage: 65

QINGDAO CARELONGPHARMATECH CO.,LTD

Tel: 0532-0532-88191853 13061484198
Email: sales@carelongchem.com
Country: China
ProdList: 403
Advantage: 57

Shanghai Topbiochem Technology Co., Ltd

Tel: 021-58170097
Email: info@topbiochem.com
Country: China
ProdList: 9452
Advantage: 58

TargetMol Chemicals Inc.

Tel: 021-021-33632979 15002134094
Fax: 021-33632979
Email: marketing@targetmol.com
Country: China
ProdList: 7854
Advantage: 58

ShangHai Caerulum Pharma Discovery Co., Ltd.

Tel: 18149758185
Email: sales-cpd@caerulumpharma.com
Country: China
ProdList: 3422
Advantage: 58

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View Lastest Price from AMG 510 manufacturers

Wuhan Haorong Biotechnology Co.,Ltd

Product: AMG 510 2252403-56-6
Price: US $0.00-0.00/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: 5000
Release date: 2023-08-07

Henan Tengmao Chemical Technology Co. LTD

Product: AMG 510 2252403-56-6
Price: US $110.00-90.00/kilogram
Min. Order: 1kilogram
Purity: 99%
Supply Ability: 10 tons/per week
Release date: 2024-01-26

Hebei Lingding Biotechnology Co., Ltd.

Product: AMG-510 2252403-56-6
Price: US $100.00/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: 9000kg/per week
Release date: 2021-06-29

2252403-56-6, AMG 510Related Search:

Baloxavir marboxil BAM7 Auranofin Atopaxar Apixaban ARV-771 Baloxavir

6-FLUORO-7-(2-FLUORO-6-HYDROXYPHENYL)-1-[4-METHYL-2-(PROPAN-2-YL)PYRIDIN-3-YL]-4-[(2S)-2-METHYL-4-(P

6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-4-[(2S)-2-methyl-4-(prop-2-enoyl)piperazin-1-yl]-1H,2H-pyrido[2,3-d]pyrimidin-2-one

AMG-510;AMG 510;AMG510

AMG 510

4-((S)-4-acryloyl-2-methylpiperazin-1-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidin-2(1H)-one

chiral AMG 510, single isomer

CPD2809

AMG-510，AMG510

AMG-510 atropisomer

Pyrido[2,3-d]pyrimidin-2(1H)-one, 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-4-[(2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-

Sotorasib (AMG-510)

AMG 510 USP/EP/BP

Sotorasib (racemate)

Sotorasib (AMG-510) racemate

Amg 510 Powder

Ras,inhibit,AMG 510,Sotorasib racemate,Inhibitor,AMG-510,Sotorasib,AMG510

6-fluoro-7-(2-fluoro-6-hydroxy-phenyl)-1-(2-isopropyl-4-methyl-3-pyridyl)-4-[(2S)-2-methyl-4-prop-2-enoyl-piperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one

Cinoxacin Impurity 4

2252403-56-6

252403-56-6

225240-56-6

GS