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SPT-IN-2

Name: SPT-IN-2
Brand: TargetMol
SKU: T218051
Rating: 4.5 (1 reviews)

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SPT-IN-2 is an orally bioavailable inhibitor of serine palmitoyltransferase (SPT), demonstrating an IC50 of 0.71 nM against human SPT2. This compound suppresses ceramide synthesis and cancer cell proliferation, while exhibiting anti-tumor efficacy, metabolic stability, and cell membrane permeability in xenograft mouse models. SPT-IN-2 efficiently blocks the de novo sphingolipid synthesis pathway, significantly reducing intracellular ceramide and 3-ketodihydrosphingosine (3-KDS) levels. It is applicable in research related to lung adenocarcinoma, acute promyelocytic leukemia, and breast cancer.

SPT-IN-2

Cas No. 2035011-97-1

Pack Size	Price	USA Stock	Global Stock	Quantity
10 mg	Inquiry	10-14 weeks	10-14 weeks
50 mg	Inquiry	10-14 weeks	10-14 weeks

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Product Introduction

Bioactivity

Description	SPT-IN-2 is an orally bioavailable inhibitor of serine palmitoyltransferase (SPT), demonstrating an IC50 of 0.71 nM against human SPT2. This compound suppresses ceramide synthesis and cancer cell proliferation, while exhibiting anti-tumor efficacy, metabolic stability, and cell membrane permeability in xenograft mouse models. SPT-IN-2 efficiently blocks the de novo sphingolipid synthesis pathway, significantly reducing intracellular ceramide and 3-ketodihydrosphingosine (3-KDS) levels. It is applicable in research related to lung adenocarcinoma, acute promyelocytic leukemia, and breast cancer.
In vitro	SPT-IN-2 (compound 5) exhibits a potent inhibitory effect on the proliferation of human acute promyelocytic leukemia PL-21 cells, with an IC₅₀ value of 4.1 nM over 5 days. The 95% confidence interval for this effect ranges from 3.4 to 4.7 nM.
In vivo	Administered at doses of SPT-IN-2 (10 mg/kg, 30 mg/kg; oral gavage; every 2 days; 2 weeks) shows significant in vivo antitumor activity in a mouse xenograft model using human acute promyelocytic leukemia PL-21 cells, effectively suppressing the tumor growth without causing notable side effects such as severe weight loss during the treatment period.

Chemical Properties

Molecular Weight	542.94
Formula	C₂₆H₂₂ClF₃N₆O₂
Cas No.	2035011-97-1
Smiles	N(C(=O)C1=CC(C(F)(F)F)=NN1C)[C@H]2[C@H](CN(C(=O)C3=CC4=C(C(Cl)=C3)N=CC=N4)CC2)C5=CC=CC=C5

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Related Tags: SPT-IN-2 in vivo | SPT-IN-2 in vitro | SPT-IN-2 formula | SPT-IN-2 molecular weight