1. JAK/STAT Signaling Stem Cell/Wnt Epigenetics
  2. STAT TET Protein
  3. NSC-370284

NSC-370284 is a selective inhibitor of ten-eleven translocation 1 (TET1) and 5-hydroxymethylcytosine (5hmC). NSC-370284 significantly inhibits the level of TET1 expression via targets STAT3/5.

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NSC-370284

NSC-370284 構造式

CAS 番号 : 116409-29-1

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 88 在庫あり
Solution
10 mM * 1 mL in DMSO USD 88 在庫あり
Solid
5 mg $80 在庫あり
10 mg $150 在庫あり
25 mg $320 在庫あり
50 mg $540 在庫あり
100 mg $940 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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製品説明

NSC-370284 is a selective inhibitor of ten-eleven translocation 1 (TET1) and 5-hydroxymethylcytosine (5hmC). NSC-370284 significantly inhibits the level of TET1 expression via targets STAT3/5[1].

IC50 & Target[1]

STAT3

 

STAT5

 

TET1

 

Cellular Effect
Cell Line Type Value Description References
U-87MG ATCC IC50
24.2 μM
Compound: NC124, NSC 370284
Cytotoxicity against human U-87 MG cells assessed as growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human U-87 MG cells assessed as growth inhibition measured after 72 hrs by MTT assay
[PMID: 32830969]
体外実験

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. NSC-370284 significantly down-regulates the level of TET1 transcription[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: AML cell lines including MONOMAC-6, THP-1, KOCL-48, and KASUMI-1.
Concentration: 0, 25, 50, 200 or 500 nM.
Incubation Time: 24 h or 48 h.
Result: Showed inhibitory for AML cells viability and TET1 transcription.
体内実験

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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (CD45.2) and B6.SJL (CD45.1) mice[1].
Dosage: 2.5 mg/kg.
Administration: Intraperitoneal injection, once daily, for 10 days.
Result: Significantly inhibited MLL-AF9 induced AML in secondary bone marrow transplantation (BMT) recipient mice.
分子量

387.43

分子式

C21H25NO6

CAS 番号
Appearance

Solid

Color

Off-white to light yellow

SMILES

OC1=C(C(N2CCCC2)C3=CC(OC)=C(OC)C(OC)=C3)C=C(OCO4)C4=C1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (258.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5811 mL 12.9056 mL 25.8111 mL 64.5278 mL
5 mM 0.5162 mL 2.5811 mL 5.1622 mL 12.9056 mL
10 mM 0.2581 mL 1.2906 mL 2.5811 mL 6.4528 mL
15 mM 0.1721 mL 0.8604 mL 1.7207 mL 4.3019 mL
20 mM 0.1291 mL 0.6453 mL 1.2906 mL 3.2264 mL
25 mM 0.1032 mL 0.5162 mL 1.0324 mL 2.5811 mL
30 mM 0.0860 mL 0.4302 mL 0.8604 mL 2.1509 mL
40 mM 0.0645 mL 0.3226 mL 0.6453 mL 1.6132 mL
50 mM 0.0516 mL 0.2581 mL 0.5162 mL 1.2906 mL
60 mM 0.0430 mL 0.2151 mL 0.4302 mL 1.0755 mL
80 mM 0.0323 mL 0.1613 mL 0.3226 mL 0.8066 mL
100 mM 0.0258 mL 0.1291 mL 0.2581 mL 0.6453 mL
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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製品名:
NSC-370284
製品番号:
HY-122258
数量:
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