AC-4-130

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).

Product information

CAS Number: 1834571-82-2

Molecular Weight: 751.20

Formula: C37H36ClF5N2O5S

Chemical Name: 4-(2-{N-[(4-chlorophenyl)methyl]2,3,4,5,6-pentafluorobenzenesulfonamido}-N-[(3,5-di-tert-butylphenyl)methyl]acetamido)benzoic acid

Smiles: CC(C)(C)C1C=C(CN(C2C=CC(=CC=2)C(O)=O)C(=O)CN(CC2C=CC(Cl)=CC=2)S(=O)(=O)C2C(F)=C(F)C(F)=C(F)C=2F)C=C(C=1)C(C)(C)C

InChiKey: NMQUSJQZQWKQBL-UHFFFAOYSA-N

InChi: InChI=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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. AC-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. AC-4-130 (0.5-2; 24 hours) reveals reduced pY-STAT5 levels both in the cytoplasm and nucleus. AC-4-130-mediated STAT5 inhibition efficiently blocks the proliferation and clonogenic growth of primary human AML cells, while healthy CD34+ cells are less sensitive.

Products are for research use only. Not for human use.