1、Product Data SheetCytochalasin BCat. No.: HY-16928CAS No.: 14930-96-2分式: CHNO分量: 479.61作靶點: Arp2/3 Complex作通路: Cytoskeleton儲存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (208.50 mM)Ethanol : 25 mg/mL (52.13 mM; Need ultrasonic)* means soluble, but saturation u

2、nknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 2.0850 mL 10.4251 mL 20.8503 mL5 mM 0.4170 mL 2.0850 mL 4.1701 mL10 mM 0.2085 mL 1.0425 mL 2.0850 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。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物

3、和給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊埾劝凑?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，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 (5.21 mM); Clear solution此案可獲得 2.5 mg/mL (5.21 mM，飽和度未知) 的澄

4、清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 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 (5.21 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (5.21 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0

5、mg/mL 的澄 DMSO 儲備液加到 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 (5.21 mM); Clear solution此案可獲得 2.5 mg/mL (5.21 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。4. 請依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% sa

6、lineSolubility: 2.5 mg/mL (5.21 mM); Clear solution此案可獲得 2.5 mg/mL (5.21 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 EtOH 儲備液加到 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。5. 請依序添加每種溶劑： 10% EtOH 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.21 mM); Clear solution此案

7、可獲得 2.5 mg/mL (5.21 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 EtOH 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。6. 請依序添加每種溶劑： 10% EtOH 90% corn oilSolubility: 2.5 mg/mL (5.21 mM); Clear solution此案可獲得 2.5 mg/mL (5.21 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 EtOH 儲備液加到 900 L

8、 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Cytochalasin B種能透過細(xì)胞的真 毒素，能夠與肌動蛋絲的有刺端結(jié)合，擾亂肌動蛋聚合物的形成，對 F-actin 的 Kd 值為 1.4-2.2 nM。IC & Target Kd: 2.2 nM (F-actin, with Mg2+), 1.4 nM (F-actin, with Mg2+/K+)1體外研究 Cytochalasin B is a cell-permeable mycotoxin binding to the barbed end of actin filaments, inhibits the en

9、longationand shortening of actin filaments, with Kds of 2.2 nM and 1.4 nM for F-actin in the presence of MgCl2 (2 mM) or MgCl2 (2 mM) plus KCl, respectively1. Cytochalasin B (0.1-10 M) shows inhibitory effect on multiple murine cancer celllines, with IC50s of 2.56 M (M109c), 10.46 M (B16BL6), 105.5

10、M (P388/ADR), 51.9 M (P388/S) and IC80s of 12.23 M (M109c), 44.86 M (B16BL6), 188.4 M (P388/ADR), 84.1 M (P388/S) after treatment for 3 h, with IC50s of 0.25 M(M109c), 0.37 M (B16F10), 0.87 M (B16BL6), and IC80s of 0.75 M (M109c), 1.21 M (B16F10), 10.41 M (B16BL6)after treatment for 4 days2. Cytocha

11、lasin B (6 M) increases the myofibrillar fragmentation index (MFI), which isattributed to the intensely breaking of myofibrillar proteins into short segments. Cytochalasin B also accelerates thedisruption of actin filaments. In addition, Cytochalasin B accelerates the transformation from F-actin to

12、G-actin,lowering the content of F-actin and significantly increasing G-actin bands during postmortem conditioning3.體內(nèi)研究 Cytochalasin B (10, 25, 50 mg/kg, i.p.) dose-dependently increases the life expectancy of Balb/c mice bearing withP388/ADR leukemias. Cytochalasin B at 50 mg/kg produces 10 % long-

13、term survival in the multidrug resistantP388/ADR cohort, and 40 % long-term survival in the drug sensitive P388/S cohort2.PROTOCOLPage 2 of 3 www.MedChemECell Assay 2 The attached cell lines M109c, B16BL6, and B16F10 are seeded at 1 to 4 104 cells/mL in 2 mL volumes in 24-wellculture plates 1 day pr

14、ior to treatment with Cytochalasin B. The suspension culture of P388/ADR cells is seeded at 5 104 cells/mL and allowed to grow overnight before Cytochalasin B treatment. Cells are treated with Cytochalasin Bfor 3 h, as well as 2, 3, or 4 days. In the case of continuous exposure for 2, 3, or 4 days,

15、attached cells are trypsinizedand counted with a hemacytometer. Leukemia cell suspensions are counted with a Coulter Counter. In the case ofshort-term exposure, cells are washed twice with fresh medium, then trypsinized (except for P388/ADR cells),reseeded, and allowed to regrow for 3 days, at which

16、 time they are counted. Growth results are calculated as thenumber of cells generated above the seeding density compared to the untreated control cells and graphicallypresented as percent of control increase2.MCE has not independently confirmed the accuracy of these methods. They are for reference o

17、nly.Animal Mice2Administration 2 For chemotherapy testing, Balb/c mice under isoflurane anesthesia are challenged with 2 105 trypan blue negativeP388/S or P388/ADR cells subcutaneously (s.c.) in a volume of 200 L. Untreated mice are kept in order to determinethe lethality of the challenge without ch

18、emotherapeutic intervention. Long-term survival is defined as challengedmice that survive the duration of the observation period. Cytochalasins B and D are prepared in suspension form in 2% carboxymethyl cellulose 1 % tween 20 (CMC/Tw) for intraperitoneal (i.p.) administration. The congeners or thev

19、ehicle are administered to leukemia-challenged mice on Days 1-8 following the initial challenge2.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 Nat Commun. 2019 Sep 4;10(1):3981.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Theodoropoulos PA, et al. Cytochalasin B may shorten actin filaments by a mechanism