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ChemicalBook > Product Catalogue >Biochemical Engineering >Inhibitors >DNA damage >PARP inhibitors >PF-01367338

PF-01367338

PF-01367338 Structure
  • ₹0
  • Product name: PF-01367338
  • CAS: 459868-92-9
  • MF: C19H21FN3O5P
  • MW: 421.37
  • EINECS:-0
  • MDL Number:MFCD17010269
  • Synonyms:AG-014699;AG-014699;PF-01367338;PF-01367338;AG14699;8-Fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-6H-pyrrolo[4,3,2-ef][2]benzazepin-6-one phosphate;Rucaparib (AG-014699 , PF-01367338);Rucaparib phosphate;AG-014699 (Rucaparib)
Manufacturer Product number Product description Packaging Price Updated Buy

Properties

Melting point :>173°C (dec.)
storage temp. :Sealed in dry,Room Temperature
solubility :Soluble in DMSO (up to 25 mg/ml).
form :Yellow solid.
color :Yellow
Stability :Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

Safety Information

Symbol(GHS): GHS hazard pictogramsGHS hazard pictograms
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H226 Flammable liquid and vapour Flammable liquids Category 3 Warning
H315 Causes skin irritation Skin corrosion/irritation Category 2 Warning GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 Causes serious eye irritation Serious eye damage/eye irritation Category 2A Warning GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
Precautionary statements:
P210 Keep away from heat/sparks/open flames/hot surfaces. — No smoking.
P233 Keep container tightly closed.
P240 Ground/bond container and receiving equipment.
P241 Use explosion-proof electrical/ventilating/lighting/…/equipment.
P242 Use only non-sparking tools.
P243 Take precautionary measures against static discharge.
P264 Wash hands thoroughly after handling.
P264 Wash skin thouroughly after handling.
P280 Wear protective gloves/protective clothing/eye protection/face protection.
P303+P361+P353 IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.
P305+P351+P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313 IF SKIN irritation occurs: Get medical advice/attention.
P337+P313 IF eye irritation persists: Get medical advice/attention.
P370+P378 In case of fire: Use … for extinction.
P403+P235 Store in a well-ventilated place. Keep cool.
P501 Dispose of contents/container to..…

Description

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. Inhibition of PARP activity has been linked to synthetic lethality in cells with mutations in BRCA1 or BRCA2 and is used as a therapeutic strategy to selectively target cancers. Rucaparib is a potent, cell-permeable inhibitor of PARP-1 (Ki = <5 nM) that is used in clinical therapy to sensitize cancer cells to chemotherapy. Rucaparib inactivates PARP activity in cells with homologous recombination DNA repair pathway mutations at LC50 values ranging from 1.3-5.5 μM. At 25 mg/kg, rucaparib arrests tumor growth in mice bearing epigenetically silenced BRCA1 UACC3199 xenograft tumors. It has been shown to increase efficacy of temozolomide in medulloblastoma cells and xenografts. Rucaparib (phosphate) is the phosphate salt of rucaparib and has improved aqueous solubility.

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