1446261-61-5

Basic information

• Product Name: (R)-methyl 9-fluoro-11b-methyl-6-oxo-2,3,5,6,11,11b-hexahydro-1H-indolizino[8,7-b]indole-7-carboxylate
• Synonyms: (R)-methyl 9-fluoro-11b-methyl-6-oxo-2,3,5,6,11,11b-hexahydro-1H-indolizino[8,7-b]indole-7-carboxylate;methyl (R)-9-fluoro-11b-methyl-6-oxo-2,3,5,6,11,11b-hexahydro-1H-indolizino[8,7-b]indole-7-carboxylate
• CAS NO: 1446261-61-5
• Molecular Formula: C17H17FN2O3
• Molecular Weight: 316.3268832
• Mol File: 1446261-61-5.mol
• Article Data: 8

Chemical Properties

• Appearance: /
• CAS DataBase Reference: (R)-methyl 9-fluoro-11b-methyl-6-oxo-2,3,5,6,11,11b-hexahydro-1H-indolizino[8,7-b]indole-7-carboxylate(CAS DataBase Reference)
• NIST Chemistry Reference: (R)-methyl 9-fluoro-11b-methyl-6-oxo-2,3,5,6,11,11b-hexahydro-1H-indolizino[8,7-b]indole-7-carboxylate(1446261-61-5)
• EPA Substance Registry System: (R)-methyl 9-fluoro-11b-methyl-6-oxo-2,3,5,6,11,11b-hexahydro-1H-indolizino[8,7-b]indole-7-carboxylate(1446261-61-5)

Safety Data

• Hazardous Substances Data: 1446261-61-5(Hazardous Substances Data)

Usage

General Description

(R)-methyl 9-fluoro-11b-methyl-6-oxo-2,3,5,6,11,11b-hexahydro-1H-indolizino[8,7-b]indole-7-carboxylate is a complex chemical compound with a long chemical name. It is a derivative of indolizino[8,7-b]indole, containing a methyl group, a fluoro group, and a carboxylate group. (R)-methyl 9-fluoro-11b-methyl-6-oxo-2,3,5,6,11,11b-hexahydro-1H-indolizino[8,7-b]indole-7-carboxylate is likely a synthetic organic molecule with potential pharmaceutical or industrial applications. The specific properties and uses of this compound would depend on its exact structure and function, which may be determined through further research and analysis.

Upstream product

• 1446261-69-3 (R)-benzyl 2-ethynyl-2-methylpyrrolidine-1-carboxylate 
• 220060-08-2 (R)-2-methylpyrrolidine-2-carboxylic acid methyl ester hydrochloride 
• 1330286-50-4 (3S,7aR)-3-(trichloromethyl)tetrahydro-1H,3H-pyrrolo[1,2-c]oxazol-1-one 
• 344-25-2 D-Prolin 
• 2086689-87-2 C₁₃H₂₁NO₂ 
• 2086689-87-2 tert-butyl 2-(2-ethynyl-2-methylpyrrolidin-1-yl)acetate 
• 872-32-2 2-methyl-1H-pyrroline 
• 1446261-60-4 (R)-methyl 6-fluoro-2-(1-(2-methoxy-2-oxoethyl)-2-methylpyrrolidin-2-yl)-1H-indole-4-carboxylate 
• 1446261-59-1 (R)-methyl 6-fluoro-2-(2-methyl-1-(2,2,2-trifluoroacetyl)pyrrolidin-2-yl)-1H-indole-4-carboxylate 
• 1446261-58-0 (R)-methyl 6-fluoro-2-(2-methyl-1-(2,2,2-trifluoroacetyl)pyrrolidin-2-yl)-1H-indole-4-carboxylate 
• 1446261-57-9 (R)-benzyl 2-((4-fluoro-2-(methoxycarbonyl)-6-(2,2,2-trifluoroacetamido)phenyl)ethynyl)-2-methylpyrrolidine-1-carboxylate 
• 1446261-56-8 methyl 2-bromo-5-fluoro-3-(2,2,2-trifluoroacetamido)-benzoate 
• 1342063-52-8 methyl 3-amino-2-bromo-5-fluorobenzoate 
• 75-75-2 methanesulfonic acid 

Downstream Products

• 1446261-44-4 (10aR)-2-fluoro-5,8,9,10,10a,11-hexahydro-10a-methyl-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(7H)-one 

Relevant articles and documents

Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development

Poly (ADP-ribose) polymerase (PARP) plays a significant role in DNA repair responses; therefore, this enzyme is targeted by PARP inhibitors in cancer therapy. Here we have developed a number of fused tetra- or pentacyclic dihydrodiazepinoindolone derivatives with excellent PARP enzymatic and cellular PARylation inhibition activities. These efforts led to the identification of pamiparib (BGB-290, 139), which displays excellent PARP-1 and PARP-2 inhibition with IC50 of 1.3 and 0.9 nM, respectively. In a cellular PARylation assay, this compound inhibits PARP activity with IC50 = 0.2 nM. Cocrystal of pamiparib shows similar binding sites with PARP with other PARP inhibitors, but pamiparib is not a P-gp substrate and shows excellent drug metabolism and pharmacokinetics (DMPK) properties with significant brain penetration (17-19%, mice). The compound is currently being investigated in phase III clinical trials as a maintenance therapy in platinum-sensitive ovarian cancer and gastric cancer.

CRYSTALLINE FORMS OF SALTS OF FUSED TERA OR PENTA-CYCLIC DIHYDRODIAZEPINOCARAZOLONES, AND USES THEREOF

Disclosed herein are salts of (R) -2-fluoro-10a-methyl-7, 8, 9, 10, 10a, 11-hexahydro-5, 6, 7a, 11-tetraazacyclohepta [def] cyclopenta [a] fluoren-4 (5H) -one, and crystalline forms (polymorphs) thereof. Also disclosed herein are methods of preparing those crystalline forms, and methods of using at least one of those crystalline forms in treating a cancer responsive to inhibition of PARP, especially a cancer associated with BRCA1/2 mutant activities or other HR deficiencies, in a subject.

FUSED TETRA OR PENTA-CYCLIC DIHYDRODIAZEPINOCARBAZOLONES AS PARP INHIBITORS

Provided are certain fused tetra or penta-cyclic compounds and salts thereof, compositions thereof, and methods of use thereof.