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別名: NSC-49842, Vincaleukoblastine, 29060-LE 中文名稱:硫酸長春堿
Vinblastine sulfate抑制微管形成和nAChR活性,在無細胞實驗的測定中,IC50為8.9 μM。Vinblastine sulfate 可誘導自噬和凋亡。
Vinblastine sulfate Chemical Structure
CAS: 143-67-9
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
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rat REF52 cells | Function assay | 0.1 μM | 30 mins | Induction of microtubule depolymerization in rat REF52 cells at 0.1 uM after 30 mins by fluorescence assay | 23947826 |
K562 cell | Proliferation assay | 48 h | Antiproliferative activity against human K562 cells after 48 hrs, IC50=0.001 μM | 19220018 | |
ACHN cells | Cytotoxicity assay | 48 h | Cytotoxicity against human ACHN cells after 48 hrs by SRB assay, IC50=22.7 μM | 19467877 | |
A375 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human A375 cells after 48 hrs by SRB assay, IC50=7.2 μM | 19467877 | |
C32 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human C32 cells after 48 hrs by SRB assay, IC50=3 μM | 19467877 | |
LNCAP cells | Cytotoxicity assay | 48 h | Cytotoxicity against human LNCAP cells after 48 hrs by SRB assay, IC50=29.3 μM | 19467877 | |
Huh-7D12 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human Huh-7D12 cells after 48 hrs by SRB assay, IC50=45.6 μM | 19467877 | |
COR-L23 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human COR-L23 cells after 48 hrs by SRB assay, IC50=45.5 μM | 19467877 | |
142BR cells | Cytotoxicity assay | 48 h | Cytotoxicity against human 142BR cells after 48 hrs by SRB assay, IC50=37.6 μM | 19467877 | |
HT-29 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human HT-29 cells after 48 hrs by MTS assay, IC50=0.55 μM | 21920762 | |
A549 cells | Proliferation assay | 48 h | Antiproliferative activity against human A549 cells after 48 hrs by MTS assay, IC50=2.36 μM | 22546674 | |
DU145 cells | Proliferation assay | 48 h | Antiproliferative activity against human DU145 cells after 48 hrs by MTS assay, IC50=4.25 μM | 22546674 | |
SK-MEL-5 cells | Proliferation assay | 48 h | Antiproliferative activity against human SK-MEL-5 cells after 48 hrs by MTS assay, IC50=1.74 μM | 22546674 | |
HepG2 cells | Proliferation assay | 48 h | Antiproliferative activity against human HepG2 cells after 48 hrs by MTS assay, IC50=0.16 μM | 22546674 | |
HT-29 cells | Proliferation assay | 48 h | Antiproliferative activity against human HT-29 cells after 48 hrs by MTS assay, IC50=11.18 μM | 22546674 | |
MCF7 cells | Proliferation assay | 48 h | Antiproliferative activity against human MCF7 cells after 48 hrs by MTS assay, IC50=24.08 μM | 22546674 | |
MDA-MB-231 cells | Proliferation assay | 48 h | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTS assay, IC50=31.52 μM | 22546674 | |
HepG2 cells | Cytotoxicity assay | 72 h | Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.056 μM | 23708010 | |
HepG2 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.019 μM | 23708010 | |
K562 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.016 μM | 23708010 | |
MDA-MB-231 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.0083 μM | 23708010 | |
MCF7 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.007 μM | 23708010 | |
UACC903 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human UACC903 cells after 48 hrs by MTS assay, IC50=1.65 μM | 21920762 | |
BxPC3 cells | Proliferation assay | 48 h | Antiproliferative activity against human BxPC3 cells after 48 hrs by MTS assay, IC50=1.13 μM | 22546674 | |
COLO 320 human colorectal carcinoma cell line | Function assay | In vitro concentration required to kill 50% of COLO 320 human colorectal carcinoma cell line, EC50=0.08 μM | 12361397 | ||
LNCaP human prostate cancer cell line | Function assay | In vitro concentration required to kill 50% of LNCaP human prostate cancer cell line, EC50=0.5 μM | 12361397 | ||
K562 cell | Growth inhibition assay | In vitro inhibitory concentration against human chronic myelogenous leukemia K562 cell growth, IC50=0.001 μM | 12852768 | ||
T47D cells | Function assay | In vitro concentration required to kill 50% of T47D human breast ductal carcinoma cell line, EC50=0.08 μM | 12361397 | ||
SCL6 cells | Cytotoxicity assay | Cytotoxicity against human SCL6 cells by MTT assay, ED50=6.1 Μm | 12880314 | ||
SCL9 | Cytotoxicity assay | Cytotoxicity against human SCL9 cells by MTT assay, ED=5.3 μM | 12880314 | ||
KATO III cells | Cytotoxicity assay | Cytotoxicity against human KATO III cells by MTT assay, ED50=6.1 μM | 12880314 | ||
NUGC4 cells | Cytotoxicity assay | Cytotoxicity against human NUGC4 cells by MTT assay, ED50=5.3 μM | 12880314 | ||
K562 cells | Function assay | Inhibition of tubulin polymerization in human K562 cells, IC50=0.13 μM | 20546980 | ||
點擊查看更多細胞系數(shù)據(jù) |
產(chǎn)品描述 | Vinblastine sulfate抑制微管形成和nAChR活性,在無細胞實驗的測定中,IC50為8.9 μM。Vinblastine sulfate 可誘導自噬和凋亡。 | ||
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靶點 |
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體外研究(In Vitro) | ||||
體外研究活性 | Vinblastine的平均終末半衰期為14.3小時。Vinblastine加入到新鮮分離的大鼠肝細胞,可迅速穿透到細胞當中[3]。Vinblastine抑制由腎上腺髓質素誘導的血管生成反應,還可引起M期阻滯[4]。在特定濃度下,vinblastine能顯著增加微核單核細胞的數(shù)量[2]。 | |||
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細胞實驗 | 細胞系 | 中國倉鼠卵巢細胞(CHO) | ||
濃度 | 1% (v/v) (dissolved in DMSO) | |||
孵育時間 | 3 h | |||
方法 | 6孔細胞培養(yǎng)板,每孔細胞密度為5×104 cells/mL,懸浮于3 mL培養(yǎng)基中。向其中加入vinblastine孵育3小時,生長21小時后進行后續(xù)檢測。 |
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實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
Western blot | ERK / p-ERK / Mcl-1 / Bad / Bid / Noxa p-JNK / c-Caspase-7 / c-PARP p-eIF2 GRP78 | 20371726 | ||
Immunofluorescence | α-tubulin / Acetyl tubulin | 30120268 | ||
Growth inhibition assay | Cell viability | 27114800 |
體內研究(In Vivo) | ||
體內研究活性 | Vinblastine作為抗癌劑被廣泛運用,但具有一些意外的副作用[6]。Vinblastine和RAP在低濃度下的結合使用,可在體內得到比較滿意的抗血管形成作用[4]。在臨床使用劑量下,vinblastine抑制CEM細胞中的微管蛋白的棕櫚?;?sup>[5]。 |
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NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
---|---|---|---|---|---|
NCT06381570 | Recruiting | Low-grade Glioma |
Daniel Morgenstern|The Hospital for Sick Children |
March 21 2024 | Early Phase 1 |
分子量 | 909.05 | 分子式 | C46H58N4O9.H2SO4 |
CAS號 | 143-67-9 | SDF | Download Vinblastine sulfate SDF |
Smiles | CCC1(CC2CC(C3=C(CCN(C2)C1)C4=CC=CC=C4N3)(C5=C(C=C6C(=C5)C78CCN9C7C(C=CC9)(C(C(C8N6C)(C(=O)OC)O)OC(=O)C)CC)OC)C(=O)OC)O.OS(=O)(=O)O | ||
儲存條件(自收到貨起) | |||
體外溶解度 |
DMSO : 100 mg/mL ( (110.0 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Water : 50 mg/mL (55.0 mM) Ethanol : Insoluble |
摩爾濃度計算器 |
體內溶解度 現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內配方計算器 |
動物體內配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)
計算結果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);
體內配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
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