| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
STAT3 STAT5 TET1
TET1 (ten-eleven translocation 1), STAT3, and STAT5. NSC-370284 targets STAT3/5 to suppress TET1 transcription, thereby reducing TET1 expression and 5-hydroxymethylcytosine (5hmC) modification. By inhibiting STAT3/5 DNA binding at the TET1 promoter, the compound suppresses TET1 expression and inhibits cancer cell viability. |
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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].
In vitro, NSC-370284 (0-500 nM; 24 h or 48 h) inhibits the viability of MONOMAC-6, THP-1, KOCL-48 and KASUMI-1 acute myeloid leukemia (AML) cells via targeting STAT3/5. It suppresses STAT3-dependent transcription with IC50 values in the low-micromolar range (~2-6 μM) in cell-based reporter assays. The compound significantly and selectively suppresses the viability of AML cells with high levels of TET1 expression. |
| 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].
In vivo, NSC-370284 (2.5 mg/kg; i.p., once daily for 10 days) improves the pathological morphologies in peripheral blood (PB), bone marrow (BM), spleen, and liver tissues in MLL-AF9 acute myeloid leukemia (AML) mice model. The compound significantly and selectively suppresses the viability of AML cells with high TET1 expression both in vitro and in vivo. |
| Enzyme Assay |
STAT3/5 inhibition is assessed using cell-free binding assays and STAT3-dependent reporter assays. NSC-370284 directly binds to and inhibits STAT3/5. TET1 expression levels are measured by qRT-PCR and Western blot in treated cells to confirm target engagement and pathway modulation.
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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. AML cell lines with high TET1 expression (e.g., MONOMAC-6, THP-1, KOCL-48, KASUMI-1) are cultured and treated with NSC-370284 at concentrations ranging from 0-500 nM for 24-48 hours. Cell viability is assessed by CellTiter-Glo or MTT assays. TET1 expression is measured by qRT-PCR and Western blot. 5hmC levels are quantified by ELISA or dot blot assays to confirm TET1 inhibition. |
| 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. MLL-AF9 acute myeloid leukemia (AML) mice model is treated with NSC-370284 at 2.5 mg/kg via intraperitoneal injection once daily for 10 days. Pathological morphologies in peripheral blood (PB), bone marrow (BM), spleen, and liver tissues are assessed. TET1 expression and 5hmC levels in tumor tissues are measured to confirm on-target activity. |
| ADME/Pharmacokinetics |
NSC-370284 has molecular formula C21H25NO6 and molecular weight 387.43. It is soluble in DMSO. The compound is supplied as a powder and should be stored at -20°C. Detailed pharmacokinetic parameters such as half-life, Cmax, and oral bioavailability require further characterization, though in vivo studies have been conducted via intraperitoneal administration at 2.5 mg/kg.
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| Toxicity/Toxicokinetics |
No comprehensive toxicity data are currently available for NSC-370284. In vivo studies at 2.5 mg/kg (i.p., daily for 10 days) did not report significant adverse effects. As a research-grade TET1 inhibitor, its full safety profile has not been extensively characterized. Standard preclinical toxicology studies would be necessary to evaluate its safety margin. The compound is for research use only and is not intended for human or veterinary use.
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| References | |
| Additional Infomation |
NSC-370284 is a research-grade small-molecule compound targeting TET1 via STAT3/5 inhibition. It is a selective inhibitor of TET1 transcription and 5-hydroxymethylcytosine (5hmC) modification. The compound has CAS number 116409-29-1 and purity ≥99%. It is also known as 6-(1-Pyrrolidinyl(3,4,5-trimethoxyphenyl)methyl)-1,3-benzodioxol-5-ol. It has not entered clinical trials or received FDA approval.
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| Molecular Formula |
C21H25NO6
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|---|---|
| Molecular Weight |
387.43
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| Exact Mass |
387.168
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| CAS # |
116409-29-1
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| PubChem CID |
340208
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.276g/cm3
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| Boiling Point |
515.2ºC at 760mmHg
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| Flash Point |
265.4ºC
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| Vapour Pressure |
3.09E-11mmHg at 25°C
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| Index of Refraction |
1.598
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| LogP |
3.269
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
487
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QCXGNLZKUHBIHD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H25NO6/c1-24-18-8-13(9-19(25-2)21(18)26-3)20(22-6-4-5-7-22)14-10-16-17(11-15(14)23)28-12-27-16/h8-11,20,23H,4-7,12H2,1-3H3
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| Chemical Name |
6-[pyrrolidin-1-yl-(3,4,5-trimethoxyphenyl)methyl]-1,3-benzodioxol-5-ol
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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 |
| 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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