吡啶并[2,3-d]嘧啶-2(1H)-一,6-氟-7-(2-氟-6-羟基苯基)-1-[4-甲基-2-(1-甲基乙基)-3-吡啶基]-4-[(2S)-2-甲基-4-(1-氧代-2-丙烯-1-基)-1-哌嗪基]-,(1R)-

Description

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 2252403-56-6 · C30H30F2N6O3. UNII 2B2VM6UC8G. Solubility: 1.3; Dissociation Constants: 8.06, 4.56.

Identification

Computed Descriptors

Physical & Chemical Properties

Physical description & handling notes

• Sotorasib is indicated in the treatment of adults with KRAS G12C mutant non small cell lung cancer. It has a moderate duration of action as it is given daily. Patients should be counselled regarding the risks of hepatotoxicity, interstitial lung disease and pneumonitis; and to avoid breastfeeding during treatment and up to 1 week after the last dose.

Documented Uses

• Sotorasib is indicated in the treatment of KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer (NSCLC) in adults who have received at least one prior systemic therapy. It is additionally approved in combination with [panitumumab] for the treatment of adult patients with KRAS G12C-mutated mCRC as determined by an FDA approved-test, who have received prior [fluorouracil]-, [oxaliplatin]- and [irinotecan]-based chemotherapy.
• Sotorasib is a small molecule inhibitor of the KRAS G12C mutant protein which is found in up to 13% of refractory cases of non-small cell lung cancer. Serum aminotransferase elevations are common during therapy with sotorasib, and a proportion of patients develop clinically apparent liver injury that can be severe.
• Breast Feeding; Lactation; Antineoplastic Agents; Enzyme Inhibitors
• Sotorasib is approved to treat adults whose cancer has an abnormal KRAS gene. It is used in:
• • colorectal cancer that has spread to other parts of the body. It is used with panitumumab in patients who have received chemotherapy that included a fluoropyrimidine, oxaliplatin, and irinotecan hydrochloride.
• • non-small cell lung cancer (NSCLC). It is used in patients who have received at least one other systemic therapy.¹

Synonyms

Sotorasib; AMG-510; 2296729-00-3; AMG510; Lumakras; AMG 510; Kras G12C inhibitor 9; Kras mutant-targeting AMG 510; 2B2VM6UC8G; CHEBI:178199; RefChem:56869; 2252403-56-6; AMG-510 racemate; SOTORASIB RACEMATE; Lumykras; Sotorasib [INN]

Frequently Asked Questions

What are the CAS number and molecular formula of 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 2252403-56-6; molecular formula C30H30F2N6O3; molecular weight — g/mol.

What other names is 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)- known by?

Sotorasib, AMG-510, 2296729-00-3, AMG510, Lumakras, AMG 510.

What are the key physical properties of 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)-?

Solubility: 1.3; Dissociation Constants: 8.06, 4.56.

Facts on this page are taken from PubChem (US National Library of Medicine) and Wikidata. Grade-specific data — assay, moisture, particle size, packaging, shelf life — is issued per batch on the COA and is not published here.