| Identification | Back Directory | [Name]
2-[6-(4-Chloro-phenyl)-1-Methyl-4H-3-oxa-2,5-diaza-benzo[e]azulen-4-yl]-acetaMide | [CAS]
1380087-89-7 | [Synonyms]
0610
CPI0160
CPI-0610
Pelabresib
BET bromodomain inhibitor
(4S)-6-(4-Chlorophenyl)-1-methyl-4H-isoxazolo[5,4-d][2]benzazepine-4-acetamide
2-[6-(4-Chloro-phenyl)-1-Methyl-4H-3-oxa-2,5-diaza-benzo[e]azulen-4-yl]-acetaMide
4H-Isoxazolo[5,4-d][2]benzazepine-4-acetamide, 6-(4-chlorophenyl)-1-methyl-, (4S)-
2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide | [Molecular Formula]
C20H16ClN3O2 | [MOL File]
1380087-89-7.mol | [Molecular Weight]
365.81 |
| Chemical Properties | Back Directory | [Boiling point ]
622.8±55.0 °C(Predicted) | [density ]
1.41±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (273.37 mM; Need ultrasonic) | [form ]
Powder | [pka]
16.07±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
BET Bromodomain Inhibitor has be shown to inhibit myeloma cell proliferation in clinically relevant models. | [in vivo]
Pelabresib (30-60 mg/kg; oral administration; for 28 days; MV-4-11 mouse xenograft model) treatment results in substantial suppression of tumor growth over the time period examined (41%, 80%, and 74% tumor growth inhibition, respectively), without any significant body weight loss in the animals[1]. | Animal Model: | MV-4-11 mouse xenograft model[1] | | Dosage: | 30 mg/kg once daily, 30 mg/kg twice daily, or 60 mg/kg once daily | | Administration: | Oral administration; for 28 days | | Result: | Suppressed of tumor growth, without any significant body weight loss in the animals.
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| [IC 50]
BRD4-BD1: 39 nM (IC50) |
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