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伐司朴达

选择性P糖蛋白抑制剂
规格或纯度: ≥98%
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货号 (SKU) 包装规格 是否现货 价格 数量
V127307-1mg 1mg 现货 Stock Image
V127307-5mg 5mg 现货 Stock Image
V127307-10mg 10mg 现货 Stock Image
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ABCB1 Inhibitor
main product photo

基本描述

规格或纯度 ≥98%
英文名称 Valspodar
别名 6-[(2S，4R，6E)-4-Methyl-2-(methylamino)-3-oxo-6-octenoic acid]cyclosporin D，Amdray，PSC833，[3′-Desoxy-3′-oxo-MeBmt]1-[Val]2-cyclosporin
英文别名 6-[(2S，4R，6E)-4-Methyl-2-(methylamino)-3-oxo-6-octenoic acid]cyclosporin D，Amdray，PSC833，[3′-Desoxy-3′-oxo-MeBmt]1-[Val]2-cyclosporin
生化机理 Valspodar is a P-glycoprotein (P-gp) inhibitor widely used in preclinical and clinical studies for overcoming multidrμg resistance (MDR). In rat, Valspodar showed properties of low hepatic extraction and wide distribution, similar to that of its structural analogue cyclosporine A. Administration of Valspodar to animals before mitoxantrone treatment increased the accumulation of mitoxantrone in the MDR tumors to 94% of that in the wild-type tumors. These studies have added direct in vitro and in vivo visual information on how P-gp processes anticancer compounds and how P-gp inhibitors modulate MDR in resistant cancer cells.Selective P-glycoprotein inhibitor. Cyclosporin analog. Shows chemosensitizing effects in vivo. Orally active.
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。

名称和标识符

IUPAC Name (3S,6S,9S,12R,15S,18S,21S,24S,30S,33S)-1,4,7,10,12,15,19,25,28-nonamethyl-33-[(E,2R)-2-methylhex-4-enoyl]-6,9,18,24-tetrakis(2-methylpropyl)-3,21,30-tri(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone
INCHI InChI=1S/C63H111N11O12/c1-26-27-28-41(16)53(76)52-57(80)67-49(38(10)11)61(84)68(19)33-48(75)69(20)44(29-34(2)3)56(79)66-50(39(12)13)62(85)70(21)45(30-35(4)5)55(78)64-42(17)54(77)65-43(18)58(81)71(22)46(31-36(6)7)59(82)72(23)47(32-37(8)9)60(83)73(24)51(40(14)15)63(86)74(52)25/h26-27,34-47,49-52H,28-33H2,1-25H3,(H,64,78)(H,65,77)(H,66,79)(H,67,80)/b27-26+/t41-,42+,43-,44+,45+,46+,47+,49+,50+,51+,52+/m1/s1
InChi Key YJDYDFNKCBANTM-QCWCSKBGSA-N
Canonical SMILES CC=CCC(C)C(=O)C1C(=O)NC(C(=O)N(CC(=O)N(C(C(=O)NC(C(=O)N(C(C(=O)NC(C(=O)NC(C(=O)N(C(C(=O)N(C(C(=O)N(C(C(=O)N1C)C(C)C)C)CC(C)C)C)CC(C)C)C)C)C)CC(C)C)C)C(C)C)CC(C)C)C)C)C(C)C
分子式

C63H111N11O12
PubChem CID 5281884
分子量 1214.62

化学和物理性质

溶解性 DMSO

安全信息

WGK Germany 3

靶标

Target ID 768
名称 ABCB1
缩写名 MDR1, PGP1
家族 ABCB subfamily
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 12 1280 7q21.12 ABCB1 ATP binding cassette subfamily B member 1
Mouse 12 1276 5 3.43 cM Abcb1a ATP-binding cassette, sub-family B (MDR/TAP), member 1A
Rat 2 147 18p11 Abcb1a ATP binding cassette subfamily B member 1A
Ensembl Gene ENSG00000085563 (Hs) , ENSMUSG00000040584 (Mm) , ENSRNOG00000008012 (Rn)
Entrez Gene 18671 (Mm) , 170913 (Rn) , 5243 (Hs)
OMIM 171050 (Hs)
Protein GI 25453402 (Rn) , 42741659 (Hs) , 153791547 (Mm)
UniProtKB P08183 (Hs) , P21447 (Mm)
DrugBank Target P08183 (Hs)
ChEMBL Target CHEMBL2573 (Mm) , CHEMBL4302 (Hs)

关联配体

Ligand ID 11745
名称 valspodar
别名 3'-keto-Bmt(1)-Val(2)-cyclosporin A
类别 Peptide
学名 4-amino-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide
生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价 Valspodar is a cyclosporin analogue. It inhibits the multidrug resistance efflux pump/transporter, p-glycoprotein (ABCB1) and via this mechanism can reverse cancer cell resistance to chemotherapeutics in cancers that overexpress ABCB1 . Valspodar does not induce the immunosuppressive effects of cyclosporin A.
单字母多肽序列
三字母多肽序列
翻译后修饰
化学修饰
临床描述 RATIONALE: Drugs used in chemotherapy use different ways to stop tumor cells from dividing so they stop growing or die. Some tumors become resistant to chemotherapy drugs. Combining PSC 833 with chemotherapy may reduce resistance to the drug, and allow more tumor cells to be killed. It is not yet known whether combination chemotherapy plus PSC 833 is more effective than combination chemotherapy alone in treating patients with relapsed or refractory multiple myeloma. PURPOSE: Randomized phase III trial to compare the effectiveness of combination chemotherapy with or without PSC 833 in treating patients with relapsed or refractory multiple myeloma.
RATIONALE: Drugs used in chemotherapy use different ways to stop tumor cells from dividing so they stop growing or die. Combining more than one drug may kill more tumor cells. PURPOSE: Randomized phase II trial to compare the effectiveness of paclitaxel with or without PSC 833 in treating patients with metastatic breast cancer.
Randomized phase III trial to compare the effectiveness of combination chemotherapy with or without PSC 833 followed by interleukin-2 or no further therapy in treating older patients who have acute myeloid leukemia. Some cancers become resistant to chemotherapy drugs. Combining PSC 833 with more than one chemotherapy drug may reduce resistance to the drugs and allow the cancer cells to be killed. Combining interleukin-2 with combination chemotherapy plus PSC 833 may kill more cancer cells.
来源公司 Eastern Cooperative Oncology Group
City of Hope Medical Center
National Cancer Institute (NCI)

参考文献

1. Loor F.  (1999)  Valspodar: current status and perspectives..  Expert Opin Investig Drugs,  8  (6):  (807-35).  [PMID:15992133]
2. Ellegaard AM et al..  (2016)  Repurposing Cationic Amphiphilic Antihistamines for Cancer Treatment..  EBioMedicine,  9  ():  (130-9).  [PMID:27333030]

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