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Pamiparib

CAT: 0013-GTR19163204-02Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19163204-02Size:200 mg
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Description
Pamiparib (BGB-290, BGB290) is a highly potent, selective and brain penetrant PARP1/2 inhibitor with potent anti-tumor activity.Ovarian Cancer Phase 2 Clinical (In Vitro) :Pamiparib shows potent DNA-trapping activity with an IC50 of 13 nM. In the cellular assays, Pamiparib inhibits intracellular PAR formation with an IC50 of 0.24 nM. Tumor cell lines with homologous recombination defects are profoundly sensitive to Pamiparib. Pamiparib is highly active both in vitro and in vivo in BRCA mutant tumors. (In Vivo) :Pamiparib suppresses PARP activity in patient-derived glioblastoma multiforme and small-cell-lung cancer xenografts, and potentiates the effects of Temozolamide. In vivo activities of Pamiparib, and its combination activity with chemotherapies in patient biopsy derived small cell lung cancer (SCLC) xenograft models.
CAS Number
1446261-44-4
Product Name Alternative
BGB-290 | BGB 290
Purity
>98% (HPLC)
Solubility
DMSO : 83.3 mg/mL 279.24 mM
Smiles
CC12CCCN1CC3=NNC (=O) C4=C5C3=C2NC5=CC (=C4) F
Molecular Formula
C16H15FN4O
Molecular Weight
298.32
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
(10aR) -2-fluoro-10a-methyl-5,8,9,10,10a,11-hexahydro-5,6,7a,11- tetraazacyclohepta[def]cyclopenta[a]fluoren-4 (7H) -one

Chemical Information

Pamiparib

Pamiparib is under investigation in clinical trial NCT03933761 (Pamiparib in Fusion Positive, Reversion Negative High Grade Serous Ovarian Cancer or Carcinosarcoma With BRCA1/2 Gene Mutations If Progression on Substrate Poly ADP Ribose Polymerase Inhibitbor (PARPI) or Chemotherapy).

CAS Number1446261-44-4
PubChem CID135565554
IUPAC Name(2R)-14-fluoro-2-methyl-6,9,10,19-tetrazapentacyclo[14.2.1.02,6.08,18.012,17]nonadeca-1(18),8,12(17),13,15-pentaen-11-one
Molecular FormulaC16H15FN4O
Molecular Weight298.31
XLogP1.6
Topological Polar Surface Area60.5
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count4
Rotatable Bond Count0
Heavy Atom Count22
Formal Charge0
Complexity566
SMILES
C[C@]12CCCN1CC3=NNC(=O)C4=C5C3=C2NC5=CC(=C4)F
InChI
InChI=1S/C16H15FN4O/c1-16-3-2-4-21(16)7-11-13-12-9(15(22)20-19-11)5-8(17)6-10(12)18-14(13)16/h5-6,18H,2-4,7H2,1H3,(H,20,22)/t16-/m1/s1
InChIKey
DENYZIUJOTUUNY-MRXNPFEDSA-N
Chemical Structure
2D Structure
2D structure of Pamiparib
CAS: 1446261-44-4
CID: 135565554
Formula: C16H15FN4O
MW: 298.31
Interactive 3D Structure
Loading 3D structure...
Computed Properties
PropertyValue
Molecular Weight298.31
XLogP31.6
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count4
Rotatable Bond Count0
Exact Mass298.12298928
Monoisotopic Mass298.12298928
Topological Polar Surface Area60.5 Ų
Heavy Atom Count22
Formal Charge0
Complexity566
Isotope Atom Count0
Defined Atom Stereocenter Count1
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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