1. PI3K/Akt/mTOR
  2. PI3K
  3. SAR-260301

SAR-260301 

Cat. No.: HY-15837 Purity: 99.74%
Handling Instructions

SAR-260301 is a selective PI3Kβ inhibitor with an IC50 of 23 nM.

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

SAR-260301 Chemical Structure

SAR-260301 Chemical Structure

CAS No. : 1260612-13-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 143 In-stock
Estimated Time of Arrival: December 31
5 mg USD 130 In-stock
Estimated Time of Arrival: December 31
10 mg USD 230 In-stock
Estimated Time of Arrival: December 31
25 mg USD 490 In-stock
Estimated Time of Arrival: December 31
50 mg USD 880 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1550 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

SAR-260301 is a selective PI3Kβ inhibitor with an IC50 of 23 nM.

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)

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].

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 (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, 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].

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 : 125 mg/mL (352.71 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

  • 2.

    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

  • 3.

    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

*All of the co-solvents are provided by MCE.
References
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].

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].

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

References
Molecular Weight

354.40

Formula

C₁₉H₂₂N₄O₃

CAS No.

1260612-13-2

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
SAR-260301
Cat. No.:
HY-15837
Quantity:

SAR-260301

Cat. No.: HY-15837