JR-AB2-011 B

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JR-AB2-011 是一种选择性 mTORC2 抑制剂，IC50 值为 0.36 μM。JR-AB2-011 通过阻断 Rictor-mTOR 联合体 (Ki: 0.19 μM) 抑制 mTORC2 活性。JR-AB2-011 具有抗多形性胶质母细胞瘤 (GBM) 的活性。

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.

Apoptosis Analysis 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 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.

Animal Model:LN229 cells in female C.B.-17-scid (Taconic) mice 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.

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PI3K/Akt/mTOR signaling

mTOR

mTOR

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2411853-34-2

398.28

C17H14Cl2FN3OS

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 62.5 mg/mL (156.92 mM; 超声助溶 )

CC1CN(C(=O)Nc2ccc(Cl)c(Cl)c2)\C(S1)=N\c1ccc(F)cc1

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(-20℃)

With Ice Pack

≥ 2 years