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
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)
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.
N-Bromosuccinimide Price
- Product number
- BA172505
- Product name
- AMG 510
- Packaging
- 5mg
- Price
- $105
- Updated
- 2021/12/16
- Product number
- BA172505
- Product name
- AMG 510
- Packaging
- 10mg
- Price
- $190
- Updated
- 2021/12/16
- Product number
- CS-0091978
- Product name
- Sotorasib(racemate)
- Purity
- 98.99%
- Packaging
- 10mg
- Price
- $200
- Updated
- 2021/12/16
- Product number
- 0113EN
- Product name
- CID137278711
- Packaging
- 10mg
- Price
- $306
- Updated
- 2021/12/16
- Product number
- BA172505
- Product name
- AMG 510
- Packaging
- 25mg
- Price
- $425
- Updated
- 2021/12/16
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
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View Lastest Price from AMG 510 manufacturers
- 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
- Product
- Lazertinib 2252403-56-6
- Price
- US $90.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 200000pcs
- Release date
- 2021-10-28
- 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