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SBI-581

Name: SBI-581
Brand: TargetMol
SKU: T61663
Rating: 4.5 (1 reviews)

(Synonyms: SBI581, SBI 581) Copy Product Info

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Synonyms: SBI581, SBI 581

Catalog No. T61663 Copy Product Info

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SBI-581 is an orally active, selective inhibitor of the serine/threonine kinase TAO3 with an IC₅₀ value of 42 nM and antitumor activity. SBI-581 promotes the accumulation of TKS5α in RAB11-positive vesicles and inhibits the formation of invasive pseudopods, thereby suppressing the invasive and migratory capabilities of tumor cells. The pharmacokinetic profile of SBI-581 following intraperitoneal administration in mice is reasonable.

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Appearance:Solid

Color:Orange

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Product Introduction

Bioactivity

Description	SBI-581 is an orally active, selective inhibitor of the serine/threonine kinase TAO3 with an IC₅₀ value of 42 nM and antitumor activity. SBI-581 promotes the accumulation of TKS5α in RAB11-positive vesicles and inhibits the formation of invasive pseudopods, thereby suppressing the invasive and migratory capabilities of tumor cells. The pharmacokinetic profile of SBI-581 following intraperitoneal administration in mice is reasonable.
Targets & IC50	TAO3:42 nM
In vitro	Methods: C8161.9 (human melanoma cells) were treated with SBI-581 (100 nM) for 2 days, and tumor spheroid size was assessed using phalloidin labeling. Results: SBI-581 significantly inhibited tumor spheroid growth. [1] Method: SBI-581 (1 μmol/L) was added to ECA109 and KYSE150 cells and incubated for 24 h; apoptosis was assessed by flow cytometry. Results: SBI-581 effectively induced apoptosis in ECA109 and KYSE150 cells. [2]
In vivo	Methods: To investigate the in vivo antitumor effects of SBI-581, a subcutaneous C8161.9 tumor model was established in nude mice. Following tumor formation, intraperitoneal administration (10 mg/kg/day) was initiated once daily for 10 consecutive days. Results: SBI-581 significantly inhibited tumor growth (volume reduction of approximately 70%) without affecting body weight. [1] Methods: To investigate the efficacy of the combination therapy of SBI-581 and cisplatin, a tumor model was established by subcutaneous inoculation of ECA109 cells into BALB/c nude mice. After tumor formation, intraperitoneal administration of SBI-581 (10 mg/kg/day) and cisplatin (3 mg/kg every 2 days) was initiated and continued for 14 days. Results: SBI-581 effectively inhibited tumor growth as a single agent, and the combination with cisplatin produced a stronger effect.[2]
Synonyms	SBI581, SBI 581

Chemical Properties

Molecular Weight	383.44
Formula	C₂₄H₂₁N₃O₂
Smiles	OC1(C#CC2=CC=CC(NC/3=O)=C2C3=C\C4=CC5=C(C=CC=C5)N4)CCNCC1

Storage & Solubility Information

Storage

Keep away from moisture,Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 40 mg/mL (104.32 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6080 mL	13.0398 mL	26.0797 mL	130.3985 mL
5 mM	0.5216 mL	2.6080 mL	5.2159 mL	26.0797 mL
10 mM	0.2608 mL	1.3040 mL	2.6080 mL	13.0398 mL
20 mM	0.1304 mL	0.6520 mL	1.3040 mL	6.5199 mL
50 mM	0.0522 mL	0.2608 mL	0.5216 mL	2.6080 mL
100 mM	0.0261 mL	0.1304 mL	0.2608 mL	1.3040 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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.