| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
STAT3 STAT5 TET1
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|---|---|
| ln Vitro |
NSC-370284 (0-500 nM; 24 h or 48 h) suppresses the viability of acute myeloid leukemia (AML) cells MONOMAC-6, THP-1, KOCL-48, and KASUMI-1 by targeting STAT3/5. NSC-370284 drastically reduces the transcription levels of TET1 [1].
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| ln Vivo |
In an MLL-AF9 acute myeloid leukemia (AML) mice model, NSC-370284 (2.5 mg/kg; i.p. once daily for 10 days) improved liver tissue, spleen, bone marrow, and peripheral blood (PB). Pathomorphological aspects [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: AML cell lines including MONOMAC-6, THP-1, KOCL-48, and KASUMI -1. Tested Concentrations: 0, 25, 50, 200 or 500 nM. Incubation Duration: 24 h or 48 h. Experimental Results: demonstrated inhibitory for AML cells viability and TET1 transcription. |
| Animal Protocol |
Animal/Disease Models: C57BL/6 (CD45.2) and B6.SJL (CD45.1) mice[1].
Doses: 2.5 mg/kg. Route of Administration: intraperitoneal (ip)injection, one time/day, for 10 days. Experimental Results: Dramatically inhibited MLL-AF9 induced AML in secondary bone marrow transplantation (BMT) recipient mice. |
| References |
[1]. Jiang X, et al. Targeted inhibition of STAT/TET1 axis as a therapeutic strategy for acute myeloid leukemia. Nat Commun. 2017 Dec 13;8(1):2099.
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| Molecular Formula |
C21H25NO6
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|---|---|
| Molecular Weight |
387.43
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| CAS # |
116409-29-1
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| SMILES |
COC1=CC(C(C2=CC3OCOC=3C=C2O)N2CCCC2)=CC(OC)=C1OC
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| 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)
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| Solubility (In Vitro) |
DMSO : 100 mg/mL (258.11 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.45 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.45 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5811 mL | 12.9056 mL | 25.8111 mL | |
| 5 mM | 0.5162 mL | 2.5811 mL | 5.1622 mL | |
| 10 mM | 0.2581 mL | 1.2906 mL | 2.5811 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.
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