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STF-083010

CAS No. : 307543-71-1

MCE 站：STF-083010

产品活性：STF-083010 是一种 IRE1α 特异性抑制剂。在内质网应激后，STF-083010 抑制 Ire1 内切核酸酶活性，而不影响其激酶活性。

研究领域：Cell Cycle/DNA Damage

作用靶点：IRE1

In Vitro: STF-083010 shows cytostatic ａnd cytotoxic activity in a dose- ａnd time-dependent manner. Treatment with STF-083010 shows significant antimyeloma activity in model human multiple myeloma (MM) xenografts. RPMI 8226 human MM cells grown as tumor xenografts are treated in NSG mice. Intraperitoneal injection of STF-083010 alone (day 1, day 8) significantly inhibits the growth of these tumors. STF-083010 is an IRE1α-specific inhibitor. Four pancreatic cancer cell lines (Panc0403, Panc1005, BxPc3, MiaPaCa2) are treated with different combination of Bortezomib (10 or 50 nM) ａnd STF (10 or 50 μM). The normalized isobologram analysis demonstrates synergistic activity between 10 μM STF ａnd either 10 or 50 nM bortezomib in all four cell lines. Moreover, a higher concentration of STF (50 μM) attains synergy after addition of bortezomib either at a concentration of 10 nM when tested against BxPc3 cells, at a concentration of 50 nM against Panc1005 cells, ａnd at either 10 or 50 nM against Panc0403 cells. STF-083010 (50 μM) suppresses the growth of p53-deficient human cancer cells.

In Vivo: Treatment with STF-083010 reduces the viability of HCT116 p53^-/- cells by approximately 20% compared with that of HCT116 p53^-/-cells. Administration of STF-083010 to tumors induced by HCT116 p53^-/- cells significantly reduces tumor volume ａnd weight by 75% ａnd 73% at the endpoint, respectively.

相关产品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Endoplasmic Reticulum Stress Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Sunitinib  |  4μ8C  |  KIRA6  |  Kira8  |  Toyocamycin  |  APY29  |  GSK2850163  |  MKC8866  |  MKC3946  |  B I09  |  6-Bromo-2-hydroxy-3-methoxybenzaldehyde  |  MKC9989  |  3,6-DMAD hydrochloride  |  IRE1α kinase-IN-1  |  IRE1α kinase-IN-2  |  KIRA-7

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