A potent

Rucaparib (phosphate) – 1 mg

Brand:
Cayman
CAS:
459868-92-9
Storage:
-20
UN-No:
Non-Hazardous - /

Poly(ADP-ribose) polymerases (PARPs) are activated by DNA single- and double-strand breaks and promote repair of DNA damage through the relaxation of chromatin and recruitment of other repair proteins.{20554,20553,20549} Inhibition of PARP activity has been linked to synthetic lethality in cells with mutations in BRCA1 or BRCA2{20680} and is used as a therapeutic strategy to selectively target cancers.{20677} Rucaparib is a potent, cell-permeable inhibitor of PARP1 (Ki = 50 values ranging from 1.3-5.5 μM.{20679} At 25 mg/kg, rucaparib arrests tumor growth in mice bearing epigenetically silenced BRCA1 UACC3199 xenograft tumors.{20679} It has been shown to increase efficacy of temozolomide in medulloblastoma cells and xenografts.{20678} Rucaparib (phosphate) is the phosphate salt of rucaparib (Item No. 15643) and has improved aqueous solubility.  

 

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SKU: 11570 - 1 mg Category:

Description

A potent, cell-permeable inhibitor of PARP1 (Ki = 50s = 1.3-5.5 μM); arrests tumor growth in mice bearing epigenetically silenced BRCA1 UACC3199 xenograft tumors

Formal name: 8-fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-6H-pyrrolo[4,3,2-ef][2]benzazepin-6-one, phosphate

Synonyms:  AG-014699|PF-01367338

Molecular weight: 421.4

CAS: 459868-92-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|DNA Repair Enzymes||Research Area|Cancer|DNA Damage and Repair|PARP

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