PLX51107 ( PLX 51107 )

产品货号. M12420 CAS No. 1627929-55-8

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

PLX51107
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

PLX51107 is a novel structurally distinct BET bromodomain inhibitor that inhibits all four BET family proteins.
产品描述

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
同义词

PLX 51107
通路

Chromatin/Epigenetic
靶点

Bromodomain
受体

Bromodomain
研究领域

Cancer
适应症

Blood cancer

CAS Number

1627929-55-8
分子量

438.49
分子式

C26H22N4O3
纯度

>98%(HPLC)
溶解度

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
化学全称

(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.

计算器

产品手册

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