2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. SPT-IN-2

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.

For research use only. We do not sell to patients.

SPT-IN-2

SPT-IN-2 Chemical Structure

CAS No. : 2035011-97-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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SPT-IN-2 Related Antibodies

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ACAT1 ACAT2 MGAT2 ACAT DGAT1 DGAT2

  • Biological Activity

  • Purity & Documentation

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Description

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[1].

Cellular Effect
Cell Line Type Value Description References
HCC4006 IC50
11 nM
Compound: 143
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
[PMID: 38621327]
In Vitro

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.

SPT-IN-2 Related Antibodies

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[1]

Cell Line: PL-21 cell
Concentration: 4.1 nM
Incubation Time: 5 days
Result: Exerted potent proliferation-inhibitory effects.
Parmacokinetics
Species Dose Route Vdss CLtotal Cmax Tmax AUC MRT F
Mice[1] 0.1 mg/kg i.v. 750 mL/kg 507 mL/h/kg / / / / /
Mice[1] 1 mg/kg p.o. / / 282 ng/mL 1.2 h 1113 ng·h/mL 2.7 h 56 %
In Vivo

SPT-IN-2 (compound 5) (10 mg/kg, 30 mg/kg; oral administration by gavage; Q2D; 2 weeks) exhibits significant in vivo anti-tumor activity in a xenograft mouse model of human acute promyelocytic leukemia PL-21 cells, effectively inhibits the in vivo growth of xenograft tumors, and causes no obvious toxic side effects such as severe body weight loss in mice during the administration period[1].

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

Animal Model: Immunodeficient nude mice bearing human acute promyelocytic leukemia PL-21 cell xenografts
[1]
Dosage: 10 mg/kg and 30 mg/kg
Administration: Oral gavage administration, once every other day (Q2D) for 2 consecutive weeks
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.
Molecular Weight

542.94

Formula

C26H22ClF3N6O2
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8418 mL 9.2091 mL 18.4182 mL
5 mM 0.3684 mL 1.8418 mL 3.6836 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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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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 (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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.60 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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.
Purity & Documentation
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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SPT-IN-2 Related Classifications

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.

Keywords:

SPT-IN-22035011-97-1AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseserine palmitoyltransferasexenograft mouse modelacute promyelocytic leukemiaceramide synthesisbreast cancercancer cell growthlung adenocarcinomaInhibitorinhibitorinhibit

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