| 名稱 | Bendamustine hydrochloride |
| 描述 | Bendamustine hydrochloride (EP-3101) (IC50 of 50 μM) is an alkylating agent associated with DNA damage. |
| 細(xì)胞實(shí)驗(yàn) | SU-DHL-1 and SU-DHL-9 cells are preincubated for 30 minutes with either 6 mM methoxyamine or 50 μM O6-benzylguanine, inhibitors of Ape-1 base excision repair enzyme, or alkylguanyl transferase enzyme, respectively. The cells are then exposed to various concentrations of Bendamustine for 72 hours. Cytotoxicity is evaluated by the MTT viability assay and an IC50 is determined as the drug concentration that inhibited by 50% the viability value of the untreated control. Analyses are done.(Only for Reference) |
| 體外活性 | Bendamustine具有明顯的活性,單獨(dú)用25 mg/kg 作用于3種腫瘤細(xì)胞 (DoHH-2, Granta 519 和RAMOS).Bendamustine 抑制Granta 519 和RAMOS生長(zhǎng)(%TGI分別為74% 和 81%),在Granta 519(%TGD 為124%) 上的作用效果比DoHH-2或RAMOS(分別為69%和43%)高.DoHH-2最敏感,ORR為30%,且抑制69%腫瘤生長(zhǎng). |
| 體內(nèi)活性 | Bendamustine比環(huán)磷酰胺, Cisplatinum, 或卡莫司汀造成的DNA單鏈和雙鏈斷裂更廣泛也更有效。Bendamustine抑制有絲分裂檢測(cè)點(diǎn),造成有絲分裂發(fā)生巨大突變。Bendamustine 調(diào)節(jié)凋亡、 DNA修復(fù)和有絲分裂檢測(cè)到涉及的基因。Bendamustine與等摩爾劑量的 Lomustine相比,具有非常低的致畸效果。Bendamustine處理的 MCF-7/ADR細(xì)胞后,26%顯示微核化,而DMSO處理的細(xì)胞中只有6%。濃度為1 μg/mL 到50 μg/mL的 Bendamustine 單獨(dú)處理,48小時(shí)后,觀察到毒性為30.4%到94.8%,這種作用存在劑量和時(shí)間依賴性。未處理和預(yù)處理的 CLL 細(xì)胞的LD50分別為7.3 或 4.4 μg /mL。 Bendamustine 處理SU-DHL-9細(xì)胞,導(dǎo)致這些基因中的全部3個(gè)（polo樣激酶1 , Aurora 激酶 A和cyclin B1）的mRNA表達(dá)下調(diào)60% 到80%。Bendamustine 作用于非Hodgkin's 淋巴細(xì)胞,與其他烷化劑相比能夠獨(dú)特調(diào)節(jié)DNA 修復(fù)通路。髓細(xì)胞和乳腺癌細(xì)胞抗 Bendamustine,但是HL-60細(xì)胞對(duì)Bendamustine 具有適中的敏感度。 |
| 存儲(chǔ)條件 | Keep away from direct sunlight,Keep away from moisture,
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : 14 mg/mL (35.47 mM), Sonication is recommended.
10% DMSO+90% Saline : 10 mg/mL (25.33 mM), Solution.
H2O : 2 mg/mL (5.07 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.07 mM), Sonication is recommended.
DMSO : 245 mg/mL (620.69 mM), Sonication is recommended.
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| 關(guān)鍵字 | SDX105 | SDX 105 | RNASynthesis | RNA Synthesis | EP3101 | EP 3101 | DNASynthesis | DNAAlkylator | DNA Synthesis | DNA Alkylator/Crosslinker | DNA Alkylator | Crosslinker | Bendamustine | Apoptosis | antimetabolite |
| 相關(guān)產(chǎn)品 | Formamide | Urea | Guanidine hydrochloride | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Sildenafil citrate | Stavudine | Tamoxifen | Thymidine |
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