PLX51107 (OPN-51107, OPN5) | BET inhibitor

Chemical Structure : PLX51107

CAS No.: 1627929-55-8

PLX51107 (PLX-51107, OPN-51107, OPN5)

Catalog No.: PC-50010Not For Human Use, Lab Use Only.

PLX51107 (OPN-51107, OPN5) is a novel structurally distinct BET bromodomain inhibitor that inhibits all four BET family proteins BRD2, BRD3, BRD4, and BRDT with low nanomolar potency.

Packing	Price	Stock
5 mg	$98	In stock
10 mg	$158	In stock
25 mg	$278	In stock
50 mg	$458	In stock
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Biological Activity

PLX51107 (OPN-51107, OPN5) is a novel structurally distinct BET bromodomain inhibitor that inhibits all four BET family proteins BRD2, BRD3, BRD4, and BRDT with low nanomolar potency.
PLX51107 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).
PLX51107 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.
PLX51107 has sufficient potency and oral bioavailability to demonstrate in vivo efficacy in animal models of a variety of tumor types.

Physicochemical Properties

M.Wt	438.487
Formula	C26H22N4O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping	Room temperature in continental US; may vary elsewhere
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-4-(6-(3,5-dimethylisoxazol-4-yl)-1-(1-(pyridin-2-yl)ethyl)-1H-pyrrolo[3,2-b]pyridin-3-yl)benzoic acid

References

1. Ozer HG, et al. Cancer Discov. 2018 Jan 31. pii: CD-17-0902.

2. Nicole R. Grieselhuber, et al. Blood 2016 128:3941.

PLX51107 (PLX-51107, OPN-51107, OPN5)

Biological Activity

Physicochemical Properties

References

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