PLX51107
Cat. No.:YN310113
CAS No. :1627929-55-8
产品名称: | PLX51107 |
CAS No.: | 1627929-55-8 |
Chemical Name: | 4-[6-(3,5-dimethyl-4-isoxazolyl)-1-[(1S)-1-(2-pyridinyl)ethyl]-1H-pyrrolo[3,2-b]pyridin-3-yl]-benzoic acid |
Synonyms: | PLX51107,PLX 51107,PLX-51107 |
分子量: | 438.48 |
分子式: | C₂₆H₂₂N₄O₃ |
SMILES: | C[C@@H](C1=NC=CC=C1)N2C=C(C3=CC=C(C(O)=O)C=C3)C4=NC=C(C5=C(C)ON=C5C)C=C42 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | PLX51107 是一种有效的,选择性的BET抑制剂,对 BRD2,BRD3,BRD4 和 BRDT 的 BD1 结构域的亲和力Kd值分别为 1.6,2.1,1.7 和 5 nM,BD2 结构域亲和力Kd值分别为 5.9,6.2,6.1 和 120 nM;PLX51107 同时与 CBP 和 EP300 的结构域相互作用 (Kd,∼ 100 nM)。 |
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Ozer, H.G., El-Gamal, D., Powell, B., et al.BRD4 profiling identifies critical chronic lymphocytic leukemia oncogenic circuits and reveals sensitivity to PLX51107, a novel structurally distinct BET InhibitorCancer Discov.8(4),458-477(2018)
Erkes, D.A., Field, C.O., Capparelli, C., et al.The next-generation BET inhibitor, PLX51107, delays melanoma growth in a CD8-mediated mannerPigm. Cell Melanoma R.32(5),687-696(2019)