产品
编 号：F762875
分子式：C36H34ClFN6O5S
分子量：717.21
分子式：C36H34ClFN6O5S
分子量：717.21
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CAS No: 3033543-67-5
产品详情
生物活性：
HSP90/mTOR-IN-1 is a potent and orally active Hsp90 and mTOR inhibitor with IC50 values of 69 nM and 29 nM, respectively. HSP90/mTOR-IN-1 suppresses the proliferation of SW780 cells through the over-activation of the PI3K/AKT/mTOR pathway. HSP90/mTOR-IN-1 induces apoptosis and autophagy via selective Hsp90 and mTOR inhibition. HSP90/mTOR-IN-1 also has considerable in vivo anti-tumor activity. HSP90/mTOR-IN-1 can be used for researching bladder cancer.
体内研究：
HSP90/mTOR-IN-1 (30 mg/kg; PO; for 17 days) exhibits significantly superior tumor growth inhibition in J82 xenograft mice.Animal Model:Balc/c nude mice (6-8 weeks; subcutaneously injected with 1×106 cells per 100 μL of J82 cells into the mice's dorsal skin)
Dosage:30 mg/kg
Administration:PO; for 17 days
Result:Exhibited significantly superior tumor growth inhibition, and did not showed remarkable weight decline.Inhibited bladder cancer cell proliferation, induced cell apoptosis, degraded Hsp70, as well as decreased phosphorylation levels of mTOR and increased expression of LC3-II.
体外研究：
HSP90/mTOR-IN-1 (compound 17o) has antiproliferative activity against J82, T24 and SW780 cells.HSP90/mTOR-IN-1 (0.2 and 0.5 μM; 24 h) induces SW870 apoptosis in a dose-dependent manner, induces the formation of autophagosome.HSP90/mTOR-IN-1 (0.2 and 0.5 μM; 24 h) decreases the expression of several Hsp90 client proteins in SW870.
HSP90/mTOR-IN-1 is a potent and orally active Hsp90 and mTOR inhibitor with IC50 values of 69 nM and 29 nM, respectively. HSP90/mTOR-IN-1 suppresses the proliferation of SW780 cells through the over-activation of the PI3K/AKT/mTOR pathway. HSP90/mTOR-IN-1 induces apoptosis and autophagy via selective Hsp90 and mTOR inhibition. HSP90/mTOR-IN-1 also has considerable in vivo anti-tumor activity. HSP90/mTOR-IN-1 can be used for researching bladder cancer.
体内研究：
HSP90/mTOR-IN-1 (30 mg/kg; PO; for 17 days) exhibits significantly superior tumor growth inhibition in J82 xenograft mice.Animal Model:Balc/c nude mice (6-8 weeks; subcutaneously injected with 1×106 cells per 100 μL of J82 cells into the mice's dorsal skin)
Dosage:30 mg/kg
Administration:PO; for 17 days
Result:Exhibited significantly superior tumor growth inhibition, and did not showed remarkable weight decline.Inhibited bladder cancer cell proliferation, induced cell apoptosis, degraded Hsp70, as well as decreased phosphorylation levels of mTOR and increased expression of LC3-II.
体外研究：
HSP90/mTOR-IN-1 (compound 17o) has antiproliferative activity against J82, T24 and SW780 cells.HSP90/mTOR-IN-1 (0.2 and 0.5 μM; 24 h) induces SW870 apoptosis in a dose-dependent manner, induces the formation of autophagosome.HSP90/mTOR-IN-1 (0.2 and 0.5 μM; 24 h) decreases the expression of several Hsp90 client proteins in SW870.
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