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Sotorasib

Sotorasib structure

CAS No:
2296729-00-3
Formula:
C30H30F2N6O3
Chemical 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
Categories:
Active Pharmaceutical Ingredients > Antineoplastic Agents

Description

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

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.

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.

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

Sotorasib Basic Attributes

Molecular Weight：

560.6

Color/Form：

White to yellow

Characteristics

Density：

1.36±0.1 g/cm3(Predicted)

Boiling Point：

730.5±70.0 °C(Predicted)

Water Solubility：

Water : 33.33 mg/mL (59.46 mM; ultrasonic and adjust pH to 11 with NaOH)

PKA：

6.52±0.35(Predicted)

Critical Temperature & Pressure：

Store at -20°C, stored under nitrogen

Sotorasib Use and Manufacturing

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.

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Sotorasib, AMG 510 2296729-00-3

CAS No.: 2296729-00-3

Grade: Pharmaceutical Grade

Content: 99%

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CAS No.: 2296729-00-3

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