1. PI3K/Akt/mTOR
  2. mTOR
  3. JR-AB2-011

JR-AB2-011 

Cat. No.: HY-122022 Purity: 98.09%
Handling Instructions

JR-AB2-011 is a selective mTORC2 inhibitor with an IC50 value of 0.36 μM. JR-AB2-011 inhibits mTORC2 activity by blocking Rictor-mTOR association (Ki: 0.19 μM). JR-AB2-011 has anti-glioblastoma multiforme (GBM) properties.

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

JR-AB2-011 Chemical Structure

JR-AB2-011 Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 286 In-stock
Estimated Time of Arrival: December 31
5 mg USD 260 In-stock
Estimated Time of Arrival: December 31
10 mg USD 440 In-stock
Estimated Time of Arrival: December 31
25 mg USD 940 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1600 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2600 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

JR-AB2-011 is a selective mTORC2 inhibitor with an IC50 value of 0.36 μM. JR-AB2-011 inhibits mTORC2 activity by blocking Rictor-mTOR association (Ki: 0.19 μM). JR-AB2-011 has anti-glioblastoma multiforme (GBM) properties[1].

IC50 & Target[1]

mTORC2

0.36 μM (IC50)

In Vitro

JR-AB2-011 (1 μM; 24 hours) has good anti-GBM properties, blocks mTORC2 signaling and Rictor association with mTOR[1].
JR-AB2-011 (0.5-2 μM; 48 hours) displays the least toxicity to normal neurons with no significant cytotoxic effects for concentrations up to 10 mM compared to CID613034[1].

Apoptosis Analysis[1]

Cell Line: U87 GBM cells; LN229 GBM cells
Concentration: 1 μM
Incubation Time: 24 hours
Result: Had good anti-GBM properties and blocked mTORC2 signaling and Rictor association with mTOR.

Cell Cytotoxicity Assay[1]

Cell Line: Normal mature human neurons
Concentration: 0.5, 1, 2 μM
Incubation Time: 48 hours
Result: Displayed the least toxicity to normal neurons with no significant cytotoxic effects for concentrations up to 10 mM.
In Vivo

Mice receiving JR-AB2-011 (4 mg/kg; daily i.p. for 10 days; 20 mg/kg; daily i.p. for 10 days) at either dosing regimen display marked inhibition of tumor growth rate (JR-AB2-011 at 4 mg/kg/d; 74% inhibition at end of dosing period; tumor growth delay 10.0 days; JR-AB2-011 at 20 mg/kg/d; 80% inhibition at end of dosing period; tumor growth delay 12.0 days) as compared to mice receiving vehicle alone[1].

Animal Model: LN229 cells in female C.B.-17-scid (Taconic) mice[1]
Dosage: 4 mg/kg; 20 mg/kg
Administration: Daily i.p.; 10 days
Result: Either dosing regimen displayed marked inhibition of tumor growth rate as compared to mice receiving vehicle alone.
Molecular Weight

398.28

Formula

C₁₇H₁₄Cl₂FN₃OS

SMILES

ClC1=C(Cl)C=C(NC(N2/C(SC(C)C2)=N/C3=CC=C(F)C=C3)=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (156.92 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5108 mL 12.5540 mL 25.1080 mL
5 mM 0.5022 mL 2.5108 mL 5.0216 mL
10 mM 0.2511 mL 1.2554 mL 2.5108 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.22 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.22 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
JR-AB2-011
Cat. No.:
HY-122022
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