GSK778 (C007B-357460)

GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC 50 s of 75 nM ( BRD2 BD1 ), 41 nM ( BRD3 BD1 ), 41 nM ( BRD4 BD1 ), and 143 nM ( BRDT BD1 ), respectively. GSK778 phenocopies the effects of pan- BET inhibitors in cancer modelsIn VitroGSK778 抑制 BRD BD2,IC 50 分别为 3950 nM (BRD2 BD2)£‚¬1210 nM (BRD3 BD2)£‚¬5843 nM (BRD4 BD2) ¥'Å’ 17451 nM (BRDT BD2)€‚ GSK778 (0.01-10 M¯1„4€º72 ¥°¦€”¶) 抑制人原代 CD4 + T 细胞§Å¡"增殖活性¥'Å’¦Ë†¥o"§»€ ¨Æ’ž¥€º ¥­§Å¡"产生,包括 IFN³£‚¬IL-17A ¥'Å’ IL-22€‚ GSK778 (0.001-10 M¯1„4€º5 天) 对 MDA-453£‚¬MOLM-13£‚¬K562£‚¬MV4-11£‚¬THP-1 ¥'Å’ MDA-MB-231 细胞€‚ GSK778 (1000 nM¯1„4€º72 ¥°¦€”¶) 在 MV4-11£‚¬MOLM13£‚¬MDA-MB-231 ¥'Å’ MB453 细胞中¦Å '制增殖,诱å¯ç»†èƒž¥' ̈¦Å“Ÿ¥Å“¦»Å¾¥'Å’§»€ ¨Æ’ž¥€¡€¹¤o¡£‚¬' GSK778 (1000 nM¯1„4€º12 天) ©TM¤1„2Ž¥Å½Å¸¤»£¤oo AML 细胞的克隆形¦Ë†¨Æ’1„2¥Å €º£‚¬' MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: Human primary CD4 + T cell Concentration: 0.001, 0.01, 0.1, 1, 10 M Incubation Time: 72 hours Result: Inhibited the proliferative activity of the cells and the production of effector cytokines. Cell Viability AssayCell Line: MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells Concentration: 0.001, 0.01, 0.1, 1, 10 M Incubation Time: 5 days Result: Inhibited the growth and viability of human cancer cell lines. Apoptosis AnalysisCell Line: MV4-11, MOLM13, MDA-MB-231 and MB453 cells Concentration: 1000 nM Incubation Time: 72 hours Result: Inhibited cell proliferation and induced a cell cycle arrest and apoptosis.In VivoGSK778 (15 mg/kg/BID;腹腔注射 30 天) 在侵袭性 MLL-AF9 AML 模型中¦¤3„4€º¤1„4 ̃¤oŽ iBET-BD2 的生存ä˜åŠ¿ €‚ GSK778 (15 mg/kg/BID;皮下注射 14 天) ¥€¡¥°'抗匙孔血¨"蛋白 (KLH) IgM 的产生并且¨‚¬¥€”性良好 €‚ GSK778 表现出 C max (85 ng/mL)£‚¬T max (1.48 h) ¥'Å’ AUC ˆž (132 ng.h/mL) 壿œ§»TM¨ Ì„ (10 mg/kg) ¥Å½¥Å“ ̈¥°©1„4 中 €‚ MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-8 weeks female C57BL/6 mice are injected with MLL-AF9 cells Dosage: 15 mg/kg/BID Administration: I.p. injections for 30 days Result: Increased the survival rate of leukemia mice. Animal Model: Male CD1 mice Dosage: 10 mg/kg (Pharmacokinetic Analysis) Administration: P.o. administration Result: C max (85 ng/mL), T max (1.48 h); AUC ˆž (132 ng.h/mL).Form:SolidIC50& Target:BRD2 BD1 75 nM (IC 50 ) BRD3 BD1 41 nM (IC 50 ) BRD4 BD1 41 nM (IC 50 ) BRDT BD1 143 nM (IC 50 ). Specification: 0.99 Molecular Formula: C30H33N5O3 Molecular Weight: 511.61

UPC:

51323007

Condition:

New

Weight:

1.06 Ounces

HazmatClass:

No;ManufacturerName=Aladdin Scientific"

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

G648442-25mg

CAS:

2451862-42-1

Product Size:

25mg

Controlled Substances and Cyanide:

Yes