PLX51107 ( PLX 51107 )

Catalog No. M12420 CAS No. 1627929-55-8

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

PLX51107
Note

Research use only, not for human use.
Brief Description

PLX51107 is a novel structurally distinct BET bromodomain inhibitor that inhibits all four BET family proteins.
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. Blood Cancer Phase 1 Clinical
Synonyms

PLX 51107
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

Cancer
Indication

Blood cancer

CAS Number

1627929-55-8
Formula Weight

438.49
Molecular Formula

C26H22N4O3
Purity

>98%(HPLC)
Solubility

DMSO : 75 mg/mL. 171.05 mM
SMILES

O=C(O)C1=CC=C(C2=CN([C@H](C3=NC=CC=C3)C)C4=CC(C5=C(C)ON=C5C)=CN=C42)C=C1
Chemical Name

(S)-4-(6-(3,5-dimethylisoxazol-4-yl)-1-(1-(pyridin-2-yl)ethyl)-1H-pyrrolo[3,2-b]pyridin-3-yl)benzoic acid

1.Ozer HG, et al. Cancer Discov. 2018 Jan 31. pii: CD-17-0902.
2.Nicole R. Grieselhuber, et al. Blood 2016 128:3941.

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