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JR-AB2-011 is a selective mTORC2 inhibitor with an IC50 value of 0.36 μM. It inhibits mTORC2 activity by blocking Rictor-mTOR association (Ki: 0.19 μM) and exhibits cytotoxicity in glioblastoma [1].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $87 | In Stock | |
5 mg | $213 | In Stock | |
10 mg | $363 | In Stock | |
25 mg | $663 | In Stock | |
50 mg | $995 | In Stock | |
100 mg | $1,330 | In Stock | |
1 mL x 10 mM (in DMSO) | $235 | In Stock |
Description | JR-AB2-011 is a selective mTORC2 inhibitor with an IC50 value of 0.36 μM. It inhibits mTORC2 activity by blocking Rictor-mTOR association (Ki: 0.19 μM) and exhibits cytotoxicity in glioblastoma [1]. |
Targets&IC50 | mTORC2:0.36 μM |
In vitro | JR-AB2-011 (1 μM; 24 hours) shows 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 administered JR-AB2-011 through intraperitoneal injection at doses of 4 mg/kg or 20 mg/kg daily for 10 days exhibited significant suppression of tumor growth compared to those treated with a vehicle control. Specifically, the lower dose achieved a 74% reduction in tumor growth rate with a 10-day delay in tumor progression, while the higher dose resulted in an 80% reduction and a 12-day delay. This study utilized female C.B.-17-scid mice implanted with LN229 cells, demonstrating that JR-AB2-011 is potent in inhibiting tumor growth at both tested concentrations. |
Molecular Weight | 398.28 |
Formula | C17H14Cl2FN3OS |
Cas No. | 2411853-34-2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 61.5 mg/mL (154.41 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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