地拉羅司作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetDeferasiroxCat. No.: HY-17359CAS No.: 201530-41-8分式: CHNO分量: 373.36作靶點(diǎn): Bacterial; Ferroptosis作通路: Anti-infection; Apoptosis儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (267.84 mM)* means soluble, but saturation unknown.SolventMas

2、s1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 2.6784 mL 13.3919 mL 26.7838 mL5 mM 0.5357 mL 2.6784 mL 5.3568 mL10 mM 0.2678 mL 1.3392 mL 2.6784 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶?/p>

3、案都請先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.70 mM); Clear solution此案可獲得 2.5 mg/mL (6.70 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取

4、 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.70 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (6.70 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液

5、加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.70 mM); Clear solution此案可獲得 2.5 mg/mL (6.70 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Deferasirox (ICL 670)具有活性的，于治療鐵離過量的螯合劑。體外研究 In

6、 LX-2 cells treated with 50 M deferasirox for 12 h, 1(I)procollagen expression is decreased by 25%, with maximalreductions (10-fold) seen following 24-120 h of treatment. Similarly, -smooth muscle actin (SMA) expression issignificantly lower1. Deferasirox had anti-proliferative effects on HL-60 or K

7、G-1 myeloid leukemia cell lines at aconcentration as low as 5 M . The cytotoxicity is both dose and time dependent2. The viability of both EL4 cells andL1210 cells incubated with deferasirox decrease in a concentration-dependent manner3.體內(nèi)研究 The tumor is significantly smaller in the SIO mice treated

8、 with deferasirox compared with control. Mice treated withDFX showed longer survival than the other groups. Deferasirox has a survival benefit for SIO leukemia murine model in terms of iron chelation and antileukemic therapy3.PROTOCOLCell Assay 2 Deferasirox is dissolved in DMSO. HL-60 or KG-1 cells

9、 are treated with 0, 5, 10, 50 M of deferasirox for 24 or 48 h,and proliferation is determined by an MTT assay2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Murine leukemia cells are injected subcutaneously into the right flank of mice.

10、Deferasirox is dissolved inAdministration 3 distilled water and orally administered at 20 mg/kg until the cumulative dose reaches 300 mg/kg. The mice areobserved and weighed daily3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) PLoS Negl Tr

11、op Dis. 2019 Aug 20;13(8):e0007681. bioRxiv. 2019 Oct.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Sobbe A, et al. Inconsistent hepatic antifibrotic effects with the iron chelator deferasirox. J Gastroenterol Hepatol. 2015 Mar;30(3):638-45.Page 2 of 3 www.MedChemE

12、2. Kim JL, et al. The oral iron chelator deferasirox induces apoptosis in myeloid leukemia cells by targetingcaspase. Acta Haematol. 2011;126(4):241-5.3. Lee DH, et al. Deferasirox shows in vitro and in vivo antileukemic effects on murine leukemic cell lines regardless of iron status. Exp Hematol. 2013Jun;41(6):539-46.McePdfHeightCaution: Product has not been