| Identification | Back Directory | [Name]
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)- | [CAS]
2296729-00-3 | [Synonyms]
Storasib
CID 137278711
AMG-510(Sotorasib)
PYRIDO[2,3-D]PYRIMIDIN-2(1H)-ONE, 6-FLUORO-7-(2-FLUORO-6-HYDROXYPHENYL)-1-[4-METHYL-2-(1-METHYLETHYL
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
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)- | [Molecular Formula]
C30H30F2N6O3 | [MOL File]
2296729-00-3.mol | [Molecular Weight]
560.61 |
| Chemical Properties | Back Directory | [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)| | [form ]
Solid | [pka]
6.52±0.35(Predicted) | [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 |
| Hazard Information | Back Directory | [Description]
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, 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. | [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. | [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. |
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