| Identification | Back Directory | [Name]
AZ6102 | [CAS]
1645286-75-4 | [Synonyms]
AZ6102
CS-2332
AZ6102 >=98% (HPLC)
AZ-6102;AZ6102;AZ 6102
rel-2-[4-[6-[(3R,5S)-3,5-Dimethyl-1-piperazinyl]-4-methyl-3-pyridinyl]phenyl]-3,7-dihydro-7-methyl-4H-pyrrolo[2,3-d]pyrimidin-4-one
4H-Pyrrolo[2,3-d]pyrimidin-4-one, 2-[4-[6-[(3R,5S)-3,5-dimethyl-1-piperazinyl]-4-methyl-3-pyridinyl]phenyl]-3,7-dihydro-7-methyl-, rel- | [Molecular Formula]
C25H28N6O | [MDL Number]
MFCD28502279 | [MOL File]
1645286-75-4.mol | [Molecular Weight]
428.53 |
| Chemical Properties | Back Directory | [Boiling point ]
657.6±65.0 °C(Predicted) | [density ]
1.31±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
crystalline solid | [pka]
8.70±0.60(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
AZ 6102 is a a potent TNKS1/2 inhibitor that has 100-fold selectivity against other poly(ADP-ribose) polymerase (PARP) family enzymes. | [Biological Activity]
az6102 is a tnks1/2 inhibitor.inhibition of the poly(adp-ribose) polymerase (parp) catalytic domain of the tankyrases (tnks1 and tnks2) is reported to inhibit the wnt pathway by increasing stabilization of axin. the canonical wnt pathway plays a critical role in adult tissue homeostasis, embryonic development, as well as cancer. | [in vitro]
az6102 was identified as a potent tnks1/2 inhibitor with 100-fold selectivity against other parp family enzymes including parps 1, 2, and 6. in addition, az6102 showed a 5 nm ic50 against wnt pathway in dld-1 cells [1]. | [in vivo]
in animal study, az6102 was intravenously dosed to nude mice at 25 mg/kg, and the results showed that az6102 had a clearance of 24 ml/min·kg and a half-life of 4 h. the bioavailability of az6102 in mouse and rat was only moderate at 12% and 18%, respectively. in addition, az6102 was used as an intravenous probe compound to evaluate the in vivo effects of tnks1/2 inhibition on normal tissue and tumor xenografts, however, the results of such experiments have not be released so far [1]. | [IC 50]
1 and 3 nm for tnks2 and tnks1, respectively | [storage]
Store at -20°C | [References]
[1] j. w. johannes, l. almeida, b. barlaam,et al.pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathways inhibitors suitable for in vivopharmacology. acs med. chem. lett. 6, 254-259 (2015). |
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