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Purity: ≥98%
| Targets |
SR-4370 targets HDAC enzymes, including HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8. It exhibits IC50 values of 0.13 μM, 0.58 μM, 0.006 μM, 3.4 μM, and 2.3 μM for HDAC1, HDAC2, HDAC3, HDAC8, and HDAC6, respectively. It shows the highest potency against HDAC3.
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| ln Vitro |
SR-4370 is an HDAC inhibitor; its IC50 values for HDAC1, HDAC2, HDAC3, HDAC8, and HDAC6 are 0.13 μM, 0.58 μM, 0.006 μM, 2.3 μM, and 3.4 μM, respectively. The breast cancer cells (MDA-MB-231) are cytotoxic to SR-4370, with an IC50 of 12.6 μM[1].
SR-4370 is an HDAC inhibitor with IC50 values of 0.13 μM, 0.58 μM, 0.006 μM, 2.3 μM, and 3.4 μM for HDAC1, HDAC2, HDAC3, HDAC8, and HDAC6, respectively. It also functions as a latency-reversing agent (LRA) for reactivation of latent HIV-1, making it a valuable tool for HIV reservoir research. |
| ln Vivo |
In vivo activity data for SR-4370 are limited. As an HDAC inhibitor and HIV latency-reversing agent, it has potential utility in animal models of HIV infection and cancer. The compound's ability to reactivate latent HIV-1 suggests potential applications in "shock and kill" strategies for HIV cure research. Further in vivo characterization is needed.
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| Enzyme Assay |
Cell-free HDAC enzyme assays for SR-4370 utilize purified recombinant HDAC isoforms (HDAC1, HDAC2, HDAC3, HDAC6, HDAC8) and fluorescent or radiometric substrates. The deacetylation reaction is performed in the presence of increasing concentrations of the compound. Enzyme activity is measured, and IC50 values are determined from concentration-response curves.
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| Cell Assay |
HIV-1 latently infected cell lines (e.g., J-Lat cells) or primary CD4+ T cells from HIV patients are treated with SR-4370 at various concentrations. HIV-1 reactivation is assessed by measuring GFP expression (in reporter cell lines) or by quantifying HIV-1 RNA by qRT-PCR. HDAC inhibition is confirmed by assessing histone acetylation by Western blot.
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| Animal Protocol |
In vivo animal studies for SR-4370 would typically involve administration via intraperitoneal or oral routes in mouse models of HIV infection (e.g., humanized mice) or cancer xenograft models. HIV-1 reactivation in vivo would be assessed by measuring plasma viral load. Efficacy in cancer models would be evaluated by tumor growth inhibition.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SR-4370 have not been comprehensively reported. As a small molecule (MW 304.33, formula C16H16F2N4O), it is expected to have reasonable membrane permeability. The compound is soluble in DMSO. Detailed PK parameters remain to be determined.
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| Toxicity/Toxicokinetics |
Toxicity data for SR-4370 are limited. As an HDAC inhibitor, standard toxicological assessments would be required for development. HDAC inhibitors are known to have potential for gastrointestinal, hematological, and cardiac toxicities. The compound's isoform selectivity may influence its safety profile.
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| References | |
| Additional Infomation |
SR-4370 (molecular formula C16H16F2N4O, MW 304.33) is a novel HDAC inhibitor and latency-reversing agent (LRA) for reactivation of latent HIV-1. It exhibits potent inhibitory activity against HDAC1, HDAC2, HDAC3, HDAC8, and HDAC6, with the highest potency against HDAC3 (IC50 = 0.006 μM). The compound is intended for research use only.
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| Molecular Formula |
C17H18F2N2O
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| Molecular Weight |
304.34
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| Exact Mass |
304.14
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| Elemental Analysis |
C, 67.09; H, 5.96; F, 12.48; N, 9.20; O, 5.26
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| CAS # |
1816294-67-3
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| Related CAS # |
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| PubChem CID |
118418385
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| Appearance |
White to off-white solid powder
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| LogP |
4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
22
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| Complexity |
346
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCNNC(=O)C1=CC=C(C=C1)C2=C(C(=CC=C2)F)F
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| InChi Key |
OSQKWTZHYXRTBG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H18F2N2O/c1-2-3-11-20-21-17(22)13-9-7-12(8-10-13)14-5-4-6-15(18)16(14)19/h4-10,20H,2-3,11H2,1H3,(H,21,22)
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| Chemical Name |
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2858 mL | 16.4290 mL | 32.8580 mL | |
| 5 mM | 0.6572 mL | 3.2858 mL | 6.5716 mL | |
| 10 mM | 0.3286 mL | 1.6429 mL | 3.2858 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.
Domain organization of classical HDACs from yeast and humans.Nat Rev Mol Cell Biol.2008 Mar;9(3):206-18. |
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HDAC4 and homologues as signal transducers.Nat Rev Mol Cell Biol.2008 Mar;9(3):206-18. |
HDAC6 is a major deacetylase in the cytoplasm.Nat Rev Mol Cell Biol.2008 Mar;9(3):206-18. |
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