AC-4-130

AC-4-130

A651226-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

AC-4-130 is a potent STAT5 SH2 domain inhibitor. AC-4-130 directly binds to STAT5 and disrupts STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription. AC-4-130 induces cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 has anti-cancer activity and can efficiently block pathological levels of STAT5 activity in acute myeloid leukemia (AML) In Vitro AC-4-130 (0.1-100 μM; 72 hours) leads to a significant increase in apoptosis in a dose-dependent and time-dependent manner in MV4-11 or MOLM-13 cells. ?\nAC-4-130 (2, 5 μM; 72 hours) induces cell cycle arrest with an increase in G0/G1 arrested cells and a concomitant reduction in cells in S or G2/M. ?\nAC-4-130 (0.5-2; 24 hours) reveals reduced pY-STAT5 levels both in the cytoplasm and nucleus. ?\nAC-4-130-mediated STAT5 inhibition efficiently blocks the proliferation and clonogenic growth of primary human AML cells, while healthy CD34+ cells are less sensitive. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:STAT5

AC-4-130 是一种强效的 STAT5 SH2 结构域抑制剂。AC-4-130 可直接与 STAT5 结合，破坏 STAT5 的活化、二聚化、核转运和 STAT5 依赖性基因转录。AC-4-130 可诱导 FLT3-ITD 驱动的细胞周期停滞和凋亡。

1834571-82-2

C37H36ClF5N2O5S

751.20 g/mol

154701370

4-[[2-[(4-chlorophenyl)methyl-(2,3,4,5,6-pentafluorophenyl)sulfonylamino]acetyl]-[(3,5-ditert-butylphenyl)methyl]amino]benzoic acid

1S/C37H36ClF5N2O5S/c1-36(2,3)24-15-22(16-25(17-24)37(4,5)6)19-45(27-13-9-23(10-14-27)35(47)48)28(46)20-44(18-21-7-11-26(38)12-8-21)51(49,50)34-32(42)30(40)29(39)31(41)33(34)43/h7-17H,18-20H2,1-6H3,(H,47,48)

NMQUSJQZQWKQBL-UHFFFAOYSA-N

CC(C)(C)C1=CC(=CC(=C1)CN(C2=CC=C(C=C2)C(=O)O)C(=O)CN(CC3=CC=C(C=C3)Cl)S(=O)(=O)C4=C(C(=C(C(=C4F)F)F)F)F)C(C)(C)C

154701370

DMSO : 100 mg/mL (133.12 mM; Need ultrasonic)