SPT-IN-2
Based on 1 Customer Validation
SPT-IN-2 is an orally active serine palmitoyltransferase (SPT) inhibitor (with an IC50 of 0.71 nM against human SPT2). SPT-IN-2 inhibits ceramide synthesis, suppresses cancer cell growth, and exhibits in vivo anti-tumor activity, favorable metabolic stability and cell membrane permeability in xenograft mouse models. SPT-IN-2 blocks the de novo sphingolipid synthesis pathway, significantly reducing intracellular ceramide levels and the levels of 3-ketodihydrosphingosine (3-KDS), the immediate downstream product of SPT. SPT-IN-2 can be used in research related to lung adenocarcinoma, acute promyelocytic leukemia and breast cancer.
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- Purity: 99.45%
- CAS No.: 2035011-97-1
- 화학식: C26H22ClF3N6O2
- 분자량:542.94
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCC4006 | IC50 |
11 nM
Compound: 143
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Antiproliferative activity against human HCC4006 cells assessed as reduction in cell growth incubated for 24 hrs by MTT assay
Antiproliferative activity against human HCC4006 cells assessed as reduction in cell growth incubated for 24 hrs by MTT assay
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[PMID: 38621327] |
SPT-IN-2 (compound 5) (IC50 4.1 nM; 5 d) exerts potent antiproliferative effects on human acute promyelocytic leukemia PL-21 cells, with a 95% confidence interval of 3.4-4.7 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PL-21 cell
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Concentration:4.1 nM
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Incubation Time:5 days
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Result:Exerted potent proliferation-inhibitory effects.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Immunodeficient nude mice bearing human acute promyelocytic leukemia PL-21 cell xenografts
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Dosage:10 mg/kg and 30 mg/kg
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Administration:Oral gavage administration, once every other day (Q2D) for 2 consecutive weeks
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Result:Exhibited significant in vivo antitumor efficacy in the PL-21 xenograft mouse model.
Effectively suppressed the growth of xenograft tumors in vivo, and no severe body weight loss or other obvious toxic side effects were observed in the treated mice during the entire administration period.
Chemical Information
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CAS No. 2035011-97-1
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Appearance Solid
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분자량 542.94
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화학식 C26H22ClF3N6O2
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Color White to off-white
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SMILES
O=C(C1=CC(C(F)(F)F)=NN1C)N[C@H]2[C@@H](C3=CC=CC=C3)CN(CC2)C(C4=CC5=C(N=CC=N5)C(Cl)=C4)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (184.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.60 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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 | 1.8418 mL | 9.2091 mL | 18.4182 mL | 46.0456 mL |
| 5 mM | 0.3684 mL | 1.8418 mL | 3.6836 mL | 9.2091 mL | |
| 10 mM | 0.1842 mL | 0.9209 mL | 1.8418 mL | 4.6046 mL | |
| 15 mM | 0.1228 mL | 0.6139 mL | 1.2279 mL | 3.0697 mL | |
| 20 mM | 0.0921 mL | 0.4605 mL | 0.9209 mL | 2.3023 mL | |
| 25 mM | 0.0737 mL | 0.3684 mL | 0.7367 mL | 1.8418 mL | |
| 30 mM | 0.0614 mL | 0.3070 mL | 0.6139 mL | 1.5349 mL | |
| 40 mM | 0.0460 mL | 0.2302 mL | 0.4605 mL | 1.1511 mL | |
| 50 mM | 0.0368 mL | 0.1842 mL | 0.3684 mL | 0.9209 mL | |
| 60 mM | 0.0307 mL | 0.1535 mL | 0.3070 mL | 0.7674 mL | |
| 80 mM | 0.0230 mL | 0.1151 mL | 0.2302 mL | 0.5756 mL | |
| 100 mM | 0.0184 mL | 0.0921 mL | 0.1842 mL | 0.4605 mL |
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