| Bioactivity | 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[1]. |
| Invitro | HSP90/mTOR-IN-1 (compound 17o) has antiproliferative activity against J82, T24 and SW780 cells[1].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[1].HSP90/mTOR-IN-1 (0.2 and 0.5 μM; 24 h) decreases the expression of several Hsp90 client proteins in SW870[1]. Cell Proliferation Assay[1] Cell Line: |
| In Vivo | HSP90/mTOR-IN-1 (30 mg/kg; PO; for 17 days) exhibits significantly superior tumor growth inhibition in J82 xenograft mice[1]. Animal Model: |
| Name | HSP90/mTOR-IN-1 |
| Formula | C36H34ClFN6O5S |
| Molar Mass | 717.21 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Pan Z, et al. Design, synthesis, and biological evaluation of novel dual inhibitors of heat shock protein 90/mammalian target of rapamycin (Hsp90/mTOR) against bladder cancer cells. Eur J Med Chem. 2022 Aug 13;242:114674. |