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Sotorasib

Product Name
Sotorasib
CAS No.
2296729-00-3
Chemical Name
Sotorasib
Synonyms
Sotorasib;AMG-510(Sotorasib);Storasib;Sotoracib;rac AMG-510;CID 137278711;Sotorasib AMG510 AMG-510;PYRIDO[2,3-D]PYRIMIDIN-2(1H)-ONE, 6-FLUORO-7-(2-FLUORO-6-HYDROXYPHENYL)-1-[4-METHYL-2-(1-METHYLETHYL;4-(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;6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one
CBNumber
CB65475731
Molecular Formula
C30H30F2N6O3
Formula Weight
560.61
MOL File
2296729-00-3.mol
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Sotorasib 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 : 100 mg/mL (178.38 mM; Need ultrasonic)|
pka
6.52±0.35(Predicted)
form 
Solid
color 
White to yellow
Water Solubility 
Water : 33.33 mg/mL (59.46 mM; ultrasonic and adjust pH to 11 with NaOH)
InChIKey
NXQKSXLFSAEQCZ-UHFFFAOYSA-N
SMILES
O=C1N=C(N2CCN(C(=O)C=C)CC2C)C2=CC(F)=C(C3C(=CC=CC=3F)O)N=C2N1C1C(=CC=NC=1C(C)C)C
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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

ChemScene
Product number
CS-0081316
Product name
Sotorasib
Purity
99.60%
Packaging
5mg
Price
$90
Updated
2021/12/16
ChemScene
Product number
CS-0081316
Product name
Sotorasib
Purity
99.60%
Packaging
10mg
Price
$160
Updated
2021/12/16
ChemScene
Product number
CS-0081316
Product name
Sotorasib
Purity
99.60%
Packaging
50mg
Price
$480
Updated
2021/12/16
ChemScene
Product number
CS-0081316
Product name
Sotorasib
Purity
99.60%
Packaging
100mg
Price
$840
Updated
2021/12/16
DC Chemicals
Product number
DC22298
Product name
AMG-510(Sotorasib)
Purity
>99%,chiralpurity>99%
Packaging
1g
Price
$1800
Updated
2021/12/16
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Sotorasib Chemical Properties,Usage,Production

Description

Sotorasib (AMG510) is a chiral compound and a potent KRAS G12C covalent inhibitor with potential antitumor activity.

Uses

Sotorasib (AMG510) is the first KRAS (G12C) inhibitor to enter clinical development. Having shown antitumor activity in clinical trials, AMG 510 represents a potentially transformative therapy.

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.

brand name

Lumakras

General Description

Sotorasib, also known as AMG-510, is an acrylamide derived KRAS inhibitor developed by Amgen. It is indicated in the treatment of adult patients with KRAS G12C mutant non small cell lung cancer. This mutation makes up >50% of all KRAS mutations. Mutant KRAS discovered in 1982 but was not considered a druggable target until the mid-2010s. It is the first experimental KRAS inhibitor. The drug [MRTX849] is also currently being developed and has the same target. Sotorasib was granted FDA approval on 28 May 2021.

General Description

Class: non-kinase; Treatment: KRAS(G12C) NSCLC; Other name: AMG 510; Elimination half-life: 5.5 h; Protein binding = 89%

Side effects

Sotorasib may cause breathing problems that could lead to death. Get emergency medical help if you have new or worsening fever, cough, or shortness of breath.
Common side effects may include:
nausea, diarrhea;
cough;
liver problems;
pain in your bones, joints, or muscles;
tiredness;
abnormal lab tests.
For 28 patients (22%), side effects led to a pause, a reduction, or both, in the dose of sotorasib. Nine people (7%) stopped the treatment because of side effects.
www.everydayhealth.com/drugs/sotorasib

target

Primary target: KRAS(G12C)

Mode of action

Sotorasib is an orally available inhibitor of the specific KRAS mutation, p.G12C, with potential antineoplastic activity. Upon oral administration, sotorasib selectively targets, binds to and inhibits the activity of the KRAS p.G12C mutant. This may inhibit growth in KRAS p.G12C-expressing tumor cells. The KRAS p.G12C mutation is seen in some tumor cell types and plays a key role in tumor cell proliferation.

Sotorasib Preparation Products And Raw materials

Raw materials

Preparation Products

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Sotorasib Suppliers

Suzhou Ryan Pharmaceutical Technology Co., Ltd.
Tel
0512-68780025 18962125825
Email
sales@ryanchem.com
Country
China
ProdList
163
Advantage
62
Anqing Benro pharmachem Technology Co.,Ltd.
Tel
05565209906 15391842992
Email
794263564@qq.com
Country
China
ProdList
116
Advantage
58
Heading (Nanjing)Pharmtechnologies Co., Ltd.
Tel
025-58467899-832 13382406280
Fax
025-58467899
Email
liucheng@headingpharm.com
Country
China
ProdList
45
Advantage
58
Changzhou Borl Biotechnology Co.,LTD
Tel
13606124132;13656121842
Email
luyan0021@163.com
Country
China
ProdList
219
Advantage
58
Suzhou Albertchem Co.,Ltd.
Tel
0512-88968486 18012631750
Email
sales@albertchemical.com
Country
China
ProdList
285
Advantage
58
Shanghai jerryxing Biomedical Technology Co., Ltd
Tel
17721492509
Email
643638326@qq.com
Country
China
ProdList
5345
Advantage
58
Shanghai Mawei Biological Technology Co., LTD
Tel
13671830408
Email
maievbiotech@163.com
Country
China
ProdList
257
Advantage
58
Shanghai Peiling Biological Technology Co., LTD
Tel
13127581762
Email
peilingchem@sina.com
Country
China
ProdList
95
Advantage
58
Cangzhou Kangrui Medical Technology Co., LTD
Tel
18632776803
Email
355803330@qq.com
Country
China
ProdList
553
Advantage
58
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
19172
Advantage
64

2296729-00-3, SotorasibRelated Search:


  • PYRIDO[2,3-D]PYRIMIDIN-2(1H)-ONE, 6-FLUORO-7-(2-FLUORO-6-HYDROXYPHENYL)-1-[4-METHYL-2-(1-METHYLETHYL
  • 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]-, (1R)-
  • AMG-510(Sotorasib)
  • 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one
  • Storasib
  • CID 137278711
  • 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]-, (1R)- 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one
  • Sotorasib
  • 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-pi
  • (1R)-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
  • (1R)-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
  • 4-(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
  • rac AMG-510
  • Sotoracib
  • Sotorasib AMG510 AMG-510
  • 2296729-00-3
  • API
  • 2296729-00-3