Cat. No.: HY-15837

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SAR-260301

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SAR-260301 is an orally available and selective PI3Kβ inhibitor with an IC₅₀ of 23 nM.

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

Purity: 99.95%
CAS No.: 1260612-13-2
Formula: C₁₉H₂₂N₄O₃
Molecular Weight:354.40

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SAR-260301 Chemical Structure

CAS No.: 1260612-13-2

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(In Japan)

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

SAR-260301 is an orally available and selective PI3Kβ inhibitor with an IC₅₀ of 23 nM^[1]^[2].

IC₅₀ & Target^[1]

PI3Kβ

23 nM (IC₅₀)

PI3Kδ

468 nM (IC₅₀)

PI3Kα

1539 nM (IC₅₀)

PI3Kγ

10000 nM (IC₅₀)

Vps34

183 nM (IC₅₀)

PI3KC2γ

3812 nM (IC₅₀)

pAkt

49 nM (IC₅₀)

DNA-PK

2000 nM (IC₅₀)

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
PC-3	EC₅₀	0.68 μM Compound: 28, SAR260301	In vivo inhibition of PI3Kbeta in tumor of po dosed SCID mouse xenografted with PTEN-deficient human PC3 cells assessed as inhibition of Akt phosphorylation at S473 In vivo inhibition of PI3Kbeta in tumor of po dosed SCID mouse xenografted with PTEN-deficient human PC3 cells assessed as inhibition of Akt phosphorylation at S473	[PMID: 24387221]
PC-3	IC₅₀	49 nM Compound: 28, SAR260301	Inhibition of PI3Kbeta-mediated Akt phosphorylation at S473 in PTEN-deficient human PC3 cells after 0.5 to 2 hrs by Immunoblotting assay Inhibition of PI3Kbeta-mediated Akt phosphorylation at S473 in PTEN-deficient human PC3 cells after 0.5 to 2 hrs by Immunoblotting assay	[PMID: 24387221]
Sf21	IC₅₀	23 nM Compound: 28, SAR260301	Inhibition of N-terminal ploy-His-tagged human PI3Kbeta expressed in baculovirus-infected sf21 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay Inhibition of N-terminal ploy-His-tagged human PI3Kbeta expressed in baculovirus-infected sf21 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	[PMID: 24387221]
Sf9	IC₅₀	1539 nM Compound: 28, SAR260301	Inhibition of N-terminal ploy-His-tagged human PI3Kalpha expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay Inhibition of N-terminal ploy-His-tagged human PI3Kalpha expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	[PMID: 24387221]
Sf9	IC₅₀	468 nM Compound: 28, SAR260301	Inhibition of N-terminal ploy-His-tagged human PI3Kdelta expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay Inhibition of N-terminal ploy-His-tagged human PI3Kdelta expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	[PMID: 24387221]
Sf9	IC₅₀	10 μM Compound: 28, SAR260301	Inhibition of C-terminal ploy-His-tagged human PI3Kgamma expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay Inhibition of C-terminal ploy-His-tagged human PI3Kgamma expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	[PMID: 24387221]
UACC-62	EC₅₀	4.55 μM Compound: 28, SAR260301	In vivo inhibition of PI3Kbeta in tumor of po dosed SCID mouse xenografted with BRAF-V600E/PTEN-deficient human UACC62 cells assessed as inhibition of Akt phosphorylation at S473 In vivo inhibition of PI3Kbeta in tumor of po dosed SCID mouse xenografted with BRAF-V600E/PTEN-deficient human UACC62 cells assessed as inhibition of Akt phosphorylation at S473	[PMID: 24387221]
UACC-62	IC₅₀	0.06 μM Compound: 28, SAR260301	Inhibition of PI3Kbeta-mediated Akt phosphorylation at S473 in BRAF-V600E/PTEN-deficient human UACC62 cells Inhibition of PI3Kbeta-mediated Akt phosphorylation at S473 in BRAF-V600E/PTEN-deficient human UACC62 cells	[PMID: 24387221]

In Vitro

In the UACC-62 tumor cell line assay, SAR-260301 inhibits pAktS473 with a measured IC₅₀ at 0.06 μM and an estimated IC₉₀ at 2 μM^[1]. In MEF-3T3-myr-p110β mechanistic model, SAR260301 inhibits PI3Kβ-dependent proliferation/viability in low serum conditions with an IC₅₀ of 196 nM. In PTEN-deficient human prostate tumor cells, SAR260301 inhibits LNCaP cell proliferation in low and high serum conditions with IC₅₀ values of 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. 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. SAR260301 also leads to antitumor activities in PTEN-deficient/BRAF-mutant human melanoma cells, inhibiting cell proliferation with IC₄₀ values of 6.5 and 3.3 μM for UACC-62 and WM-266.4, respectively, after 4-day treatment^[2].

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

In Vivo

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 is well tolerated at the active dose, with no sign of toxicity and no body weight loss. Oral administration of SAR-260301 reveals sustained target inhibition (≥50%) of pAkt-S473 for at least 7 h. SAR-260301 has moderate terminal elimination half-life (t_1/2=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, po), mice (100 mg/kg, po), female nude rats (3 mg/kg, iv), rat (10 mg/kg, po), male beagle dogs (10 mg/kg, po))^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1260612-13-2
Appearance Solid
Molecular Weight 354.40
Formula C₁₉H₂₂N₄O₃
Color White to off-white
SMILES

O=C1N=C(CC(N2[C@@H](C)CC3=C2C=CC=C3)=O)NC(N4CCOCC4)=C1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (282.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8217 mL

14.1084 mL

28.2167 mL

5 mM

0.5643 mL

2.8217 mL

5.6433 mL

10 mM

0.2822 mL

1.4108 mL

2.8217 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 2.08 mg/mL (5.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (5.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (5.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protocol

Cell Assay^[2]

Cell proliferation is measured by quantifying intracellular ATP using CellTiter-Glo kit. Cells seeded into 96-well black microplates in complete medium, are treated with single or combined agents (e.g., SAR260301) 0.3 nM-30 μM (0.1% DMSO final concentration) for 96 hours^[2].

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

Animal Administration^[1]

Mice^[1]
SAR-260301 is evaluated for its antitumor effects in UACC-62 melanoma subcutaneous xenografts in SCID mice. Tumors are allowed to reach at least 150 mm³ before treatment, and tumor volume is measured regularly over the treatment period. Mice are treated orally with SAR-260301 at the dose of 150 mg/kg using a bidaily (BID) schedule in order to favor sustained pathway inhibition and allow comparison with the study performed in PC3 model^[1].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Certal V, et al. Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers. J Med Chem. 2014 Feb 13;57(3):903-20. [Content Brief]

[2]. Bonnevaux H, et al. Concomitant Inhibition of PI3Kβ and BRAF or MEK in PTEN-Deficient/BRAF-Mutant Melanoma Treatment: Preclinical Assessment of SAR260301 Oral PI3Kβ-Selective Inhibitor. Mol Cancer Ther. 2016 Jul;15(7):1460-71. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8217 mL	14.1084 mL	28.2167 mL	70.5418 mL
	5 mM	0.5643 mL	2.8217 mL	5.6433 mL	14.1084 mL
	10 mM	0.2822 mL	1.4108 mL	2.8217 mL	7.0542 mL
	15 mM	0.1881 mL	0.9406 mL	1.8811 mL	4.7028 mL
	20 mM	0.1411 mL	0.7054 mL	1.4108 mL	3.5271 mL
	25 mM	0.1129 mL	0.5643 mL	1.1287 mL	2.8217 mL
	30 mM	0.0941 mL	0.4703 mL	0.9406 mL	2.3514 mL
	40 mM	0.0705 mL	0.3527 mL	0.7054 mL	1.7635 mL
	50 mM	0.0564 mL	0.2822 mL	0.5643 mL	1.4108 mL
	60 mM	0.0470 mL	0.2351 mL	0.4703 mL	1.1757 mL
	80 mM	0.0353 mL	0.1764 mL	0.3527 mL	0.8818 mL
	100 mM	0.0282 mL	0.1411 mL	0.2822 mL	0.7054 mL

Keywords

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SAR-260301

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Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Lactylation Compound Library

All PI3K Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

SAR-260301 Related Classifications

Cat. No.: HY-15837