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

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 decreases the phosphorylation level of Akt, decreases MMP2 activity, thereby reducing the ability of tumor cells to migrate and invade. JR-AB2-011 also induces non-apoptotic cell death.

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

JR-AB2-011 Chemical Structure

JR-AB2-011 Chemical Structure

CAS No. : 2411853-34-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 286 In-stock
Solution
10 mM * 1 mL in DMSO USD 286 In-stock
Solid
5 mg USD 260 In-stock
10 mg USD 440 In-stock
25 mg USD 800 In-stock
50 mg USD 1280 In-stock
100 mg USD 2050 In-stock
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Based on 14 publication(s) in Google Scholar

JR-AB2-011 Related Antibodies

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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)[1].JR-AB2-011 decreases the phosphorylation level of Akt, decreases MMP2 activity, thereby reducing the ability of tumor cells to migrate and invade. JR-AB2-011 also induces non-apoptotic cell death[2].

IC50 & Target[1]

mTORC2

0.36 μM (IC50)

In Vitro

JR-AB2-011 (10 µM - 250 µM; 48h) significantly reduces the survival rate and proliferation ability of different melanoma cell lines (MelJu, MelJuso, MelIm, B16)[2].
JR-AB2-011 (50 µM, 250 µM; 48 h) decreases the phosphorylation level of Akt in MelIm cells, indicating that inhibition of mTORC2 attenuated the Ak t signaling pathway[2].
JR-AB2-011 (50 µM, 250 µM; 48-78 h) results in a significant decrease in cell survival fraction SF and a significant reduction in the migration and invasive ability of melanoma cells, which is mainly achieved by decreasing MMP2 activity[2].

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

JR-AB2-011 Related Antibodies

Western Blot Analysis[2]

Cell Line: MelJuso
Concentration: 50 µM, 250 µM
Incubation Time: 72h
Result: JR-AB2-011 significantly reduced MMP2 protein and inhibited MMP2 activity, thereby inhibiting tumor cell invasion.
In Vivo

JR-AB2-011 (20 mg/kg; i.p.; daily) reduces the size and number of liver metastases in C57BL/6N mice with injection of B16 cells. No severe side effects or weight loss[2].
JR-AB2-011 (4 mg/kg; p.o.; daily) significantly blocks the Dioscin-induced promotion of M2 macrophage polarization[3].

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

Animal Model: C57BL/6N mice with injection of B16 cells [2].
Dosage: 20 mg/kg everyday
Administration: i.p.
Result: JR-AB2-011 resulted in a significant decrease in hepatic tumor burden and metastasis load, as assessed by MRI and BLI.
Histological analysis confirmed the presence of fewer and smaller metastases in the liver of treated mice. MMP2 expression was also significantly reduced.
Animal Model: DSS (dextran sulfate sodium) induced colitis in mice [3]
Dosage: 4 mg/kg; Dioscin 160 mg/kg; daily
Administration: p.o.
Result: JR-AB2-011 significantly blocked the Dioscin-induced promotion of M2 macrophage polarization.
JR-AB2-011 inhibited the mTORC2/PPAR-γ signaling pathway, attenuating the regulatory effects of Dioscin on macrophage metabolism and polarization.
The decrease in inflammation-related biomarkers (e.g., TNF-α, IL-6, IFN-γ, etc.) was partially reversed, indicating that the anti-inflammatory effects of Dioscin were suppressed.
Molecular Weight

398.28

Formula

C17H14Cl2FN3OS
CAS No.
Appearance

Solid

Color

White to off-white

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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In Vivo:

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

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 (5.22 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (5.22 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.16%

COA (253 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5108 mL 12.5540 mL 25.1080 mL 62.7699 mL
5 mM 0.5022 mL 2.5108 mL 5.0216 mL 12.5540 mL
10 mM 0.2511 mL 1.2554 mL 2.5108 mL 6.2770 mL
15 mM 0.1674 mL 0.8369 mL 1.6739 mL 4.1847 mL
20 mM 0.1255 mL 0.6277 mL 1.2554 mL 3.1385 mL
25 mM 0.1004 mL 0.5022 mL 1.0043 mL 2.5108 mL
30 mM 0.0837 mL 0.4185 mL 0.8369 mL 2.0923 mL
40 mM 0.0628 mL 0.3138 mL 0.6277 mL 1.5692 mL
50 mM 0.0502 mL 0.2511 mL 0.5022 mL 1.2554 mL
60 mM 0.0418 mL 0.2092 mL 0.4185 mL 1.0462 mL
80 mM 0.0314 mL 0.1569 mL 0.3138 mL 0.7846 mL
100 mM 0.0251 mL 0.1255 mL 0.2511 mL 0.6277 mL
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JR-AB2-011 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JR-AB2-0112411853-34-2mTORMammalian target of RapamycinC57BL/6N mice melanoma cellMMP2AktInhibitorinhibitorinhibit

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