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Sotorasib

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Sotorasib Basic information

Product Name:
Sotorasib
Synonyms:
  • 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
CAS:
2296729-00-3
MF:
C30H30F2N6O3
MW:
560.61
Product Categories:
  • API
  • 2296729-00-3
Mol File:
2296729-00-3.mol
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Sotorasib Chemical Properties

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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Sotorasib Usage And Synthesis

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.

SotorasibSupplier

Suzhou Ryan Pharmaceutical Technology Co., Ltd. Gold
Tel
0512-68780025 18962125825
Email
sales@ryanchem.com
Anqing Benro pharmachem Technology Co.,Ltd. Gold
Tel
05565209906 15391842992
Email
794263564@qq.com
Heading (Nanjing)Pharmtechnologies Co., Ltd. Gold
Tel
025-58467899-832 13382406280
Email
liucheng@headingpharm.com
Changzhou Borl Biotechnology Co.,LTD Gold
Tel
13606124132;13656121842
Email
luyan0021@163.com
Suzhou Albertchem Co.,Ltd. Gold
Tel
0512-88968486 18012631750
Email
sales@albertchemical.com
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