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307543-71-1

中文名稱 STF 083010
英文名稱 STF 083010
CAS 307543-71-1
分子式 C15H11NO3S2
分子量 317.38
MOL 文件 307543-71-1.mol
更新日期 2024/12/12 09:51:17
307543-71-1 結構式 307543-71-1 結構式

基本信息

中文別名
IRE1抑制劑(STF-083010)
N-[(2-羥基-1-萘基)亞甲基]-2-噻吩磺酰胺
英文別名
CS-2901
CS-2595
STF 083010
STF-083010
STF083010
STF 083010
N-[(2-Hydroxy-1-naphthalenyl)methylene]-2-thiophenesulfonamide
2-Thiophenesulfonamide, N-[(2-hydroxy-1-naphthalenyl)methylene]-
(E)-N-((2-hydroxynaphthalen-1-yl)methylene)thiophene-2-sulfonamide
所屬類別
生物化工:激動劑抑制劑

物理化學性質

熔點199-201°C
沸點548.4±56.0 °C(Predicted)
密度1.40±0.1 g/cm3(Predicted)
儲存條件-20°C
溶解度DMSO:可溶,5mg/mL(澄清溶液)
酸度系數(pKa)7.31±0.50(Predicted)
形態(tài)粉末
顏色淡黃色至黃綠色
穩(wěn)定性自購買之日起 1 年內保持穩(wěn)定。 DMSO 中的溶液可在 -20° 下保存長達 3 個月。

安全數據

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302
危險品標志Xn
危險類別碼22
WGK Germany3

常見問題列表

生物活性
STF-083010 是一種 IRE1α 特異性抑制劑。在內質網應激后,STF-083010 抑制 Ire1 內切核酸酶活性,而不影響其激酶活性。
靶點

Ire1

體外研究

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.

體內研究

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.

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