Description Biological Activity Storage In vivo
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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

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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
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
Dideu Industries Group Limited
Product
AMG 510 2252403-56-6
Price
US $1.10/g
Min. Order
1g
Purity
99.9%
Supply Ability
100 Tons min
Release date
2021-08-17

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
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