PLX51107

PLX51107 is a bromodomain and extra terminal domain (BET) family protein inhibitor. It binds to bromodomain 1 (BD1) in bromodomain-containing protein 2 (BRD2), BRD3, BRD4, and BRDT (Kds = 1.6, 2.1, 1.7, and 5 nM, respectively), as well as BD2 (Kds = 5.9, 6.2, 6.1, and 120 nM, respectively). It also binds to the bromodomains of CBP and p300 (Kds = ~100 nM for both). PLX51107 (0.1-10 µM) inhibits CpG-induced proliferation of primary chronic lymphocytic leukemia (CLL) cells. In vivo, PLX51107 (0.5-10 mg/kg) inhibits Ba/F3 cell-induced splenomegaly in mice. It also reduces tumor volume and increases survival in YUMM3.3 and D4M3.A mouse syngeneic B-RAFV600E mutant melanoma models.Formal Name: 4-[6-(3,5-dimethyl-4-isoxazolyl)-1-[(1S)-1-(2-pyridinyl)ethyl]-1H-pyrrolo[3,2-b]pyridin-3-yl]-benzoic acid. CAS Number: 1627929-55-8. Molecular Formula: C26H22N4O3. Formula Weight: 438.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: >50 mg/ml. lambdamax: 227, 251, 305 nm. 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. InChi Code: InChI=1S/C26H22N4O3/c1-15-24(17(3)33-29-15)20-12-23-25(28-13-20)21(18-7-9-19(10-8-18)26(31)32)14-30(23)16(2)22-6-4-5-11-27-22/h4-14,16H,1-3H3,(H,31,32)/t16-/m0/s1. InChi Key: AMSUHYUVOVCWTP-INIZCTEOSA-N.