氟達(dá)拉濱作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetFludarabineCat. No.: HY-B0069CAS No.: 21679-14-1分式: CHFNO分量: 285.23作靶點(diǎn): Nucleoside Antimetabolite/Analog; DNA/RNA Synthesis; STAT; Apoptosis作通路: Cell Cycle/DNA Damage; JAK/STAT Signaling; Stem Cell/Wnt; Apoptosis儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month

2、溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 25 mg/mL (87.65 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 3.5059 mL 17.5297 mL 35.0594 mL5 mM 0.7012 mL 3.5059 mL 7.0119 mL10 mM 0.3506 mL 1.7530 mL 3.5059 mL請(qǐng)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(qǐng)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。-80

3、C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊?qǐng)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(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.76 mM); Cl

4、ear solution此案可獲得 2.5 mg/mL (8.76 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(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (8.76 mM); Clear solution此案可獲得 2.5 mg/mL (8.76 mM，飽和度未知) 的澄清溶液。Pag

5、e 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄均勻。DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (8.76 mM); Clear solution此案可獲得 2.5 mg/mL (8.76 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。BIOLOGI

6、CAL ACTIVITY物活性 Fludarabine (F-ara-A; NSC 118218) DNA 合成抑制劑，也抑制 STAT1 磷酸化。Fludarabine 化作代謝轉(zhuǎn)化為抗代謝藥物 F-ara-A。種前藥，通過去磷酸體外研究 Fludarabine (5 M; 48 hours) induces a decrease in p27kip1 expression4.Western Blot Analysis4Cell Line: B-CLL cellsConcentration: 5 MIncubation Time: 24 hoursResult: Induces a decr

7、ease in p27kip1 expression. The decrease in p27kip1 expression wassignificantly correlated to the extent of in vitro apoptosis.體內(nèi)研究 Fludarabine (0.8 mg/kg; i.p.; two cycles for 5 days every 2 weeks) in combination with Cyclophosphamide (400 mg/kg;i.p.; 2 weeks) decreases incidence of GVHD5.Animal Mo

8、del: F-1 mice received 105 BCL-1 leukemia cells5Dosage: 0.8 mg/kgAdministration: Intraperitoneal injection; two cycles for 5 days every 2 weeksResult: Combination with Cyclophosphamide decreased incidence of graft-versus-hostdisease (GVHD).戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Exp Clin Cancer Res. 2019 Aug 22;38(1):370. J

9、Infect. 2019 Jun 18. pii: S0163-4453(19)30187-2. J Mol Med (Berl). 2019 Aug;97(8):1183-1193. Int J Mol Sci. 2019 Feb 3;20(3). pii: E663. Antivir Res. 2020 Apr.See more customer validations on HYPERLINK www.MedChemE www.MedChemEPage 2 of 3 www.MedChemEREFERENCES1. Tournilhac O, et al. Impact of front

10、line fludarabine and cyclophosphamide combined treatment on peripheral blood stem cell mobilization in B-cellchronic lymphocytic leukemia. Blood. 2004 Jan 1;103(1):363-5. Epub 2003 Sep 11.2. Liang YB, et al. Downregulated SOCS1 expression activates the JAK1/STAT1 pathway and promotes polarization of

11、 macrophages into M1 type. Mol MedRep. 2017 Nov;16(5):6405-6411.3. Sanhes L, et al. Fludarabine-induced apoptosis of B chronic lymphocytic leukemia cells includes early cleavage of p27kip1 by caspases. Leukemia. 2003Jun;17(6):1104-11.4. Weiss L, et al. Fludarabine in combination with cyclophosphamid

12、e decreases incidence of GVHD and maintainseffective graft-versus-leukemia effectafter allogeneic stem cell transplantation in murinelymphocytic leukemia. Bone Marrow Transplant. 2003 Jan;31(1):11-5.5. Frank DA,et al. Fludarabine-induced immunosuppression is associated with inhibition of STAT1 signaling. Nat Med. 1999 Apr;5(4):444-7.McePdfHeightCaution: Product has not bee