| 名稱 | Vinblastine sulfate |
| 描述 | Vinblastine sulfate (Vincaleukoblastine sulfate salt) can inhibit the formation of microtubule, it also inhibits nAChR(IC50=8.9 uM). |
| 細(xì)胞實(shí)驗(yàn) | Six-well treatment plates are set up that contained 5 × 104 cells/mL in each well, suspended in 3 mL culture medium, and these are treated with vinblastine for 3 h followed by 21 h growth. (Only for Reference) |
| 激酶實(shí)驗(yàn) | Cell based receptor autophosphorylation assays: Autophosphorylation of PDGFR family kinase assays are cell-based enzyme-linked immunosorbent (ELISA) assays using CHO cells expressing wild-type PDGFRβ, chimeric protein PDGFRβ/c-Kit, and PDGFRβ/Flt3 which contain the extracellular and transmembrane domains of PDGFRβ and the cytoplasmic domain of c-Kit, and Flt-3. Cells are grown to confluency in 96-well microtiter plates under standard tissue culture conditions, followed by serum starvation for 16 hours. Briefly, quiescent cells are incubated at 37 °C with increasing concentrations of Tandutinib for 30 minutes followed by the addition of 8 nM PDGF-BB for 10 minutes. Cells are lysed in 100 mM Tris, pH 7.5, 750 mM NaCl, 0.5% Triton X-100, 10 mM sodium pyrophosphate, 50 mM NaF, 10 μg/mL aprotinin, 10 μg/mL leupeptin, 1 mM phenylmethylsulfonyl fluoride, 1 mM sodium vanadate, and the lysate is cleared by centrifugation at 15,000 g for 5 minutes. Clarified lysates are transferred into a second microtiter plate in which the wells are previously coated with 500 ng/well of 1B5B11 anti-PDGFRβ mAb and then incubated for 2 hours at room temperature. After washing three times with binding buffer (0.3% gelatin, 25 mM HEPES, pH 7.5, 100 mM NaCl, 0.01% Tween 20), 250 ng/mL of rabbit polyclonal anti-phosphotyrosine antibody is added and plates are incubated at 37 °C for 60 minutes. Subsequently, each well is washed three times with binding buffer and incubated with 1 μg/mL of horseradish peroxidase-conjugated anti-rabbit antibody at 37 °C for 60 minutes. Wells are washed prior to adding 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid), and the rate of substrate formation is monitored at 650 nm. |
| 體外活性 | Vinblastine的平均終末半衰期為14.3小時(shí)。在新鮮分離的大鼠肝細(xì)胞中孵育時(shí)，VLB迅速且強(qiáng)烈地滲透進(jìn)入細(xì)胞內(nèi)，這一過(guò)程很可能通過(guò)被動(dòng)擴(kuò)散機(jī)制實(shí)現(xiàn)，隨后緊密地與細(xì)胞結(jié)合[3]。Vinblastine通過(guò)抑制由腎上腺髓質(zhì)素誘導(dǎo)的血管生成反應(yīng)，同時(shí)對(duì)于有絲分裂滑移也表現(xiàn)出積極效應(yīng)，導(dǎo)致帶有細(xì)胞分裂阻滯的單核細(xì)胞中出現(xiàn)微核[4]。在產(chǎn)生約50%的細(xì)胞死亡和細(xì)胞靜止或更低濃度下，根據(jù)RPD、RICC和RCC的計(jì)算，vinblastine顯著增加了微核化的單核細(xì)胞數(shù)量[2]。 |
| 體內(nèi)活性 | Vinblastine是一種廣泛使用的抗癌化合物，但具有不希望的副作用[6]。VBL與RAP的低劑量組合對(duì)人類HCC在體內(nèi)展現(xiàn)出令人滿意的抗血管生成效果[4]。臨床相關(guān)劑量的Vinblastine在體內(nèi)抑制CEM細(xì)胞中tubulin的棕櫚酰化作用（對(duì)tubulin去棕櫚?；挠绊懀5]。 |
| 存儲(chǔ)條件 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 90.9 mg/mL (100 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
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| 關(guān)鍵字 | inhibit | Vinblastine sulfate | Vincaleukoblastine | Autophagy | Vincaleukoblastine Sulfate | Microtubule/Tubulin | Inhibitor | Vinblastine Sulfate | NSC 49842 | Vinblastine | NSC-49842 |
| 相關(guān)產(chǎn)品 | Guanidine hydrochloride | Naringin | Valproic Acid | Taurine | Gefitinib | Aceglutamide | Hydroxychloroquine | Curcumin | Stavudine | Salicylic acid | Paeonol | Sodium 4-phenylbutyrate |
| 相關(guān)庫(kù) | 抗癌活性化合物庫(kù) | 植物來(lái)源化合物庫(kù) | 抗衰老化合物庫(kù) | 中藥單體化合物庫(kù) | 疼痛相關(guān)化合物庫(kù) | 抗癌臨床化合物庫(kù) | 高通量篩選天然產(chǎn)物庫(kù) | 抗癌藥物庫(kù) |