| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
AC-4-130 targets the STAT5 (signal transducer and activator of transcription 5) SH2 domain. STAT5 is a transcription factor that plays a critical role in cell proliferation, survival, and differentiation, and is frequently hyperactivated in hematological malignancies such as acute myeloid leukemia (AML). AC-4-130 is a potent and selective inhibitor of the STAT5 SH2 domain that directly binds to STAT5, blocking its phosphorylation, dimerization, and nuclear translocation. By disrupting STAT5-dependent gene transcription, AC-4-130 reduces pathological STAT5 activity.
|
|---|---|
| ln Vitro |
Significant increases in MV4-11 or MOLM-13 cells are caused by AC-4-130 (0.1-100 μM; 72 hours) in a formulation- and time-dependent manner [1]. Cell induction cycle is triggered by AC-4-130 (2, 5 μM; 72 hours), which causes a decrease in S or G2/M phase cells and an increase in G0/G1-induced cells [1]. The cytoplasm and nucleus of AC-4-130 (0.5-2; 24 hours) cells displayed decreased pY-STAT5 levels. Primary human AML cells' ability to proliferate and develop clonally was significantly suppressed by AC-4-130-mediated suppression of STAT5, whereas healthy CD34+ cells are less susceptible [1].
In vitro, AC-4-130 is a potent and selective inhibitor of the STAT5 SH2 domain. It directly binds to STAT5, blocking its phosphorylation, dimerization, and nuclear translocation. The compound disrupts STAT5-dependent gene transcription, effectively reducing pathological STAT5 activity in AML cells. It has anticancer activity. These in vitro studies establish AC-4-130 as a potent and selective STAT5 inhibitor with potential therapeutic applications in AML. |
| ln Vivo |
In vivo activity data for AC-4-130 is limited, as the compound is primarily used as a research tool in in vitro studies. However, its mechanism of action—inhibiting STAT5 signaling—suggests potential in vivo applications in hematological malignancies. The compound could be used in animal models of AML to study the effects of STAT5 inhibition on tumor growth. However, specific in vivo protocols and results are not detailed in standard product descriptions.
|
| Enzyme Assay |
In vitro assays for AC-4-130 measure its binding to the STAT5 SH2 domain and its ability to inhibit STAT5 phosphorylation, dimerization, and nuclear translocation. Binding assays are performed using purified STAT5 SH2 domain protein and a labeled probe. Functional assays measure the inhibition of STAT5-dependent gene transcription using reporter gene assays in cells expressing STAT5. The compound's ability to inhibit STAT5 phosphorylation is assessed by Western blotting using phospho-specific antibodies.
|
| Cell Assay |
In vitro cell-based assays for AC-4-130 are conducted using AML cell lines or other cells with activated STAT5 signaling. Cells are treated with AC-4-130 at various concentrations, and the phosphorylation of STAT5 is measured by Western blotting. The expression of STAT5 target genes is measured by quantitative PCR. Cell proliferation and apoptosis are assessed using standard assays such as MTT, CellTiter-Glo, or Annexin V staining. These assays confirm that AC-4-130 inhibits STAT5 signaling and exerts anti-leukemic effects.
|
| Animal Protocol |
In vivo animal experiments for AC-4-130 would typically be conducted in mouse models of AML. In a typical study, immunodeficient mice are engrafted with human AML cells and treated with AC-4-130. Tumor growth is monitored, and the survival of the mice is recorded. The compound's ability to inhibit tumor growth and improve survival is assessed. However, specific protocols for AC-4-130 are not detailed in standard product descriptions.
|
| ADME/Pharmacokinetics |
AC-4-130 has a molecular weight of 751.21 g/mol and a molecular formula of C37H36ClF5N2O5S. It is a solid compound with a purity of ≥98% by HPLC. It is soluble in DMSO at 100 mg/mL with ultrasonic treatment. For storage, it is recommended to keep the powder at -20°C. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized. As a research compound, its stability is maintained by proper storage as a dry powder.
|
| Toxicity/Toxicokinetics |
Detailed toxicity data for AC-4-130 is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. AC-4-130 is a STAT5 inhibitor, and its toxicity would be related to its effects on STAT5-mediated signaling in normal tissues. However, comprehensive toxicological studies have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed when handling AC-4-130. Its use is limited to research applications and it is not intended for human or veterinary use.
|
| References | |
| Additional Infomation |
AC-4-130 is a research compound and is not approved for any clinical or therapeutic use. It is a potent, selective inhibitor of the STAT5 SH2 domain that directly binds to STAT5, blocking its phosphorylation, dimerization, and nuclear translocation. AC-4-130 acts by disrupting STAT5-dependent gene transcription, effectively reducing pathological STAT5 activity in acute myeloid leukemia (AML). It has anticancer activity and is a promising therapeutic candidate and a valuable tool for studying STAT5-mediated oncogenic signaling. Its mechanism of action involves inhibiting STAT5 activation and downstream signaling.
|
| Molecular Formula |
C37H36CLF5N2O5S
|
|---|---|
| Molecular Weight |
751.202165603638
|
| Exact Mass |
750.195
|
| CAS # |
1834571-82-2
|
| Related CAS # |
1834571-82-2;
|
| PubChem CID |
154701370
|
| Appearance |
Off-white to brown solid powder
|
| LogP |
9.1
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
51
|
| Complexity |
1260
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
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
|
| InChi Key |
NMQUSJQZQWKQBL-UHFFFAOYSA-N
|
| InChi Code |
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)
|
| Chemical Name |
4-(2-((N-(4-chlorobenzyl)-2,3,4,5,6-pentafluorophenyl)sulfonamido)-N-(3,5-di-tert-butylbenzyl)acetamido)benzoic acid
|
| Synonyms |
AC4130 AC-4130 AC4-130 AC-4-130
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~133.12 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3312 mL | 6.6560 mL | 13.3120 mL | |
| 5 mM | 0.2662 mL | 1.3312 mL | 2.6624 mL | |
| 10 mM | 0.1331 mL | 0.6656 mL | 1.3312 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
