Description Biological Activity Storage In vivo
ChemicalBook > CAS DataBase List > AMG 510

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;(S)-AMG-510;AMG-510,AMG510;Amg 510 Powder
CBNumber
CB24858719
Molecular Formula
C30H30F2N6O3
Formula Weight
560.59
MOL File
2252403-56-6.mol
More
Less

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)
form 
Solid
pka
6.52±0.35(Predicted)
color 
Light yellow to yellow
More
Less

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.

More
Less

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
More
Less

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

More
Less

AMG 510 Suppliers

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
2634
Advantage
58
Wuhan Bo Jin Biotechnology Co.,Ltd.
Tel
18164232327
Email
2709603029@qq.com
Country
China
ProdList
291
Advantage
58
Shanghai Mawei Biological Technology Co., LTD
Tel
13671830408
Email
maievbiotech@163.com
Country
China
ProdList
257
Advantage
58
Elucigen bio
Tel
13501719342
Email
wayne.zheng@elucigenbio.com
Country
China
ProdList
5089
Advantage
58
Beijing HwrkChemical Technology Co., Ltd
Tel
010-89508211 18501085097
Fax
010-89508210
Email
sales.bj@hwrkchemical.com
Country
China
ProdList
8415
Advantage
55
Wuhan Sunrise Technology Development Co., Ltd.
Tel
27-027-83314682 13554138826
Fax
+86 (27) 8331-4682
Email
whsrtech@vip.163.com
Country
China
ProdList
252
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
7189
Advantage
65
QINGDAO CARELONGPHARMATECH CO.,LTD
Tel
0532-0532-88191853 13061484198
Email
sales@carelongchem.com
Country
China
ProdList
411
Advantage
57
Shanghai Topbiochem Technology Co., Ltd
Tel
021-58170097
Email
info@topbiochem.com
Country
China
ProdList
9459
Advantage
58
More
Less

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
Hebei Mojin Biotechnology Co., Ltd
Product
AMG 510 2252403-56-6
Price
US $0.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
50000KG/month
Release date
2024-10-10
Qiuxian Baitai New Material Co., LTD
Product
Lazertinib 2252403-56-6
Price
US $90.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
200000pcs
Release date
2021-10-28

2252403-56-6, AMG 510Related Search:


  • 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
  • (S)-AMG-510
  • 2252403-56-6
  • 252403-56-6
  • 225240-56-6
  • GS