PXL51107
Data Sheet
For research use only. Not for human use.
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| CAS No. | 1627929-55-8 | Cat. No. | BCP28928 |
| Name | PXL51107 | ||
| Synonyms | PXL 51107 ; PXL-51107; | ||
| SMILES | C O)(=O)C1=CC=C(C2C3=NC=C(C4=C(C) | ||
| Chemical Name | |||
| Formula | C26H22N4O3 | M. Wt | 438.48 |
| Purity | 98% | Storage | Store at 4-8°C |
| Description | PLX51107 is a novel structurally distinct BET bromodomain inhibitor that inhibits all four BET family proteins BRD2, BRD3, BRD4, and BRDT with low nanomolar potency; exhibits modest preference for BD1 versus BD2 within each BET protein (Kd=1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1 and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively).potently reduces viability and proliferation of the human AML cell lines MV4-11, MOLM-13, OCI-AML3, and Kasumi-1 with IC50 of 0.17, 1.8, 0.2 and 0.2 uM, respectively; has sufficient potency and oral bioavailability to demonstrate in vivo efficacy in animal models of a variety of tumor types.PLX51107 shows significant interactions only with the bromodomains of CBP and EP300 (p300) (Kd in the 100 nM range). | ||
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