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AC-4-130

Katalog-Nr.GC62272

AC-4-130 ist ein potenter Inhibitor der STAT5-SH2-DomÄne. AC-4-130 bindet direkt an STAT5 und unterbricht die STAT5-Aktivierung, Dimerisierung, Kerntranslokation und STAT5-abhÄngige Gentranskription. AC-4-130 induziert Zellzyklusstillstand und Apoptose in FLT3-ITD-gesteuerten LeukÄmiezellen. AC-4-130 wirkt gegen Krebs und kann pathologische Werte der STAT5-AktivitÄt bei akuter myeloischer LeukÄmie (AML) wirksam blockieren.

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AC-4-130 Chemische Struktur

Cas No.: 1834571-82-2

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5 mg
225,00 $
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10 mg
342,00 $
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25 mg
675,00 $
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50 mg
1.170,00 $
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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)[1].

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[1]. 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[1]. AC-4-130 (0.5-2; 24 hours) reveals reduced pY-STAT5 levels both in the cytoplasm and nucleus[1]. 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[1].

[1]. Bettina Wingelhofer, et al. Pharmacologic inhibition of STAT5 in acute myeloid leukemia. Leukemia. 2018 May;32(5):1135-1146.

Chemical Properties

Cas No. 1834571-82-2 SDF
Formula C37H36ClF5N2O5S M.Wt 751.2
Löslichkeit Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.3312 mL 6.656 mL 13.312 mL
5 mM 0.2662 mL 1.3312 mL 2.6624 mL
10 mM 0.1331 mL 0.6656 mL 1.3312 mL
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