Shopping Cart

Your shopping cart is currently empty

SAR-260301

Name: SAR-260301
Brand: TargetMol
SKU: T16841
Price: 38 USD
Availability: InStock
Rating: 5 (10 reviews)

Copy Product Info

😃Good

Catalog No. T16841Cas No. 1260612-13-2

SAR-260301, an orally available and selective inhibitor of PI3Kβ [IC50: 23 nM].

SAR-260301

Copy Product Info

😃Good

Purity: 99.74%

Catalog No. T16841Cas No. 1260612-13-2

SAR-260301, an orally available and selective inhibitor of PI3Kβ [IC50: 23 nM].

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$38	In Stock	In Stock
5 mg	$63	In Stock	In Stock
10 mg	$94	In Stock	In Stock
25 mg	$193	In Stock	In Stock
50 mg	$293	In Stock	In Stock
100 mg	$413	In Stock	In Stock
200 mg	$582	-	In Stock
1 mL x 10 mM (in DMSO)	$68	In Stock	In Stock

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Batch Information

Select Batch

Purity:99.74%

Appearance:Solid

Color:Yellow

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	SAR-260301, an orally available and selective inhibitor of PI3Kβ [IC50: 23 nM].
Targets&IC50	PI3Kδ:468 nM, PI3KC2γ:3812 nM, PI3Kβ:23 nM, PI3Kγ:10000 nM, VPS34:183 nM, pAkt:49 nM, PI3Kα:1539 nM, DNA-PK:2000 nM
In vitro	SAR-260301 inhibits pAktS473 (a measured IC50: 0.06 μM and an estimated IC90: 2 μM), in the UACC-62 tumor cell line assay. SAR260301 inhibits PI3Kβ-dependent proliferation/viability in low serum conditions (IC50: 196 nM), in the MEF-3T3-myr-p110β mechanistic model. SAR260301 inhibits LNCaP cell proliferation in low and high serum conditions (IC50: 2.9 and 5.0 μM, respectively), after 4-day treatment, whereas it is inactive in these conditions in PC3 cells at concentrations up to 10 μM, despite target engagement). SAR260301 also leads to antitumor activities in PTEN-deficient/BRAF-mutant human melanoma cells, inhibiting cell proliferation (IC40: 6.5 and 3.3 μM for UACC-62 and WM-266.4, respectively, after 4-day treatment). After prolonged treatment, SAR260301 at 3 or 10 μM inhibits PC3 cell proliferation in low serum conditions, with a cytostatic effect achieved for 14 days, despite some cell death induction observed at 10 μM [2].
In vivo	SAR-260301 is well tolerated at the active dose, with no sign of toxicity and no bodyweight loss. SAR-260301 displays antitumor efficacy in human PTEN-deficient melanoma models in mice as a single agent. SAR-260301 treatment leads to a statistically significant tumor growth inhibition as measured by a ΔT/ΔC of 39% (p = 0.054 versus control mice) on day 15 post-tumor implantation. SAR-260301(p.o.) reveals sustained target inhibition (≥50%) of pAkt-S473 for at least 7 h. SAR-260301 has moderate terminal elimination half-life (t1/2=0.87 h, 1.4 h, 2.5 h, 0.87h, 6.9 h and 4.5 h for female SCID mice (3 mg/kg, iv), mice (10 mg/kg, p.o.), mice (100 mg/kg, p.o.), female nude rats (3 mg/kg, iv), rat (10 mg/kg, p.o.), male beagle dogs (10 mg/kg, p.o.)) [1].

Chemical Properties

Molecular Weight	354.4
Formula	C₁₉H₂₂N₄O₃
Cas No.	1260612-13-2
Smiles	C[C@H]1Cc2ccccc2N1C(=O)Cc1nc(cc(=O)[nH]1)N1CCOCC1
Relative Density.	1.38 g/cm3 (Predicted)

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.

Solubility Information

DMSO: 125 mg/mL (352.71 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (11.29 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.8217 mL	14.1084 mL	28.2167 mL	141.0835 mL
5 mM	0.5643 mL	2.8217 mL	5.6433 mL	28.2167 mL
10 mM	0.2822 mL	1.4108 mL	2.8217 mL	14.1084 mL
20 mM	0.1411 mL	0.7054 mL	1.4108 mL	7.0542 mL
50 mM	0.0564 mL	0.2822 mL	0.5643 mL	2.8217 mL
100 mM	0.0282 mL	0.1411 mL	0.2822 mL	1.4108 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

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