Methotrexate (CL-14377)

For research use only. Not for use in humans.

目录号:S1210 别名: NCI-C04671, Amethopterin, WR19039

Methotrexate (CL-14377) Chemical Structure

CAS No. 59-05-2

Methotrexate (CL14377, MTX, NCI-C04671, Amethopterin, WR19039),一种叶酸类似物,是细菌、癌细胞和正常细胞中dihydrofolate reductase(DHFR)的非选择性抑制剂,与DHFR、NADPH形成无活性的三元复合物。Methotrexate (MTX)可诱导凋亡。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1096.19 现货
RMB 974.61 现货
RMB 2776.41 现货
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客户使用Selleck生产的Methotrexate (CL-14377)发表文献55篇:

产品安全说明书

ADC Cytotoxin抑制剂选择性比较

生物活性

产品描述 Methotrexate (CL14377, MTX, NCI-C04671, Amethopterin, WR19039),一种叶酸类似物,是细菌、癌细胞和正常细胞中dihydrofolate reductase(DHFR)的非选择性抑制剂,与DHFR、NADPH形成无活性的三元复合物。Methotrexate (MTX)可诱导凋亡。
靶点
hDHFR [4]
(Activated peripheral T cells)
24 nM
体外研究

Methotrexate (0.1-10 mM)诱导体外活化的来自人类外周血的T细胞的细胞凋亡。在混合淋巴细胞反应中,Methotrexate使活化的T细胞的克隆缺失。Methotrexate能够通过CD95不依赖的途径选择性删除活化的外周血中T细胞。[1] Methotrexate通过还原性叶酸载体被细胞利用,随后在细胞内被转化为聚谷氨酸盐。Methotrexate导致体外中性粒细胞刺激的白三烯B4的产生减少。Methotrexate聚谷氨酸盐抑制5-氨基咪唑-4-氨甲酰核糖核苷 (AICAR)甲酰基转移酶,比对其他参与嘌呤生物合成的酶更加有效。Methotrexate也通过抑制体外TNF诱导的核因子κB活化而抑制TNF活性,与该因子,IκBα的一个抑制剂的降解和活化的减少部分相关,也可能与腺苷的释放有关。Methotrexate通过来自健康人体和RA患者的T细胞受体激活的T淋巴细胞抑制TNF 和IFN-γ的产生。Methotrexate的治疗与TNF-α阳性的CD4+ T 细胞显著减少,而T细胞表达的抗炎因子IL-10的数量增加有关。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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CCRF-CEM NFPXNVVHfW6ldHnvckBie3OjeR?= NW\NN21VUW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KESraInkdo9nd2yjdHWgdoVlfWO2YYPlJEhFUE[UKTDpd49t[XSnZDDmdo9uKEOFUl[tR2VOKGi3bXHuJIxmfWunbXnhJINmdGy|IHnuJIV5eGW{aX3lcpQhOSxiSVO1NEA:KDBwMECxNVgh|ryPLh?= NFm2VIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi96NU[4PFI4Lz56NU[4PFI4RC:jPh?=
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OMC-1 MkW0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV7Jcohq[mm2aX;uJI9nKGi3bXHuJG9OSy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTCyOE43OjF{IN88UU4> NH73[XY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{PDJ3OT:nQnNCVkeHUkyvZV4>
Hs-578-T M3f0c2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnTtTY5pcWKrdHnvckBw\iCqdX3hckBJey13N{itWEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOjRwN{C5O{DPxE1w MlvOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|QzPTlxJ{7TRW5ITVJ:L3G+
SNB75 NEnDcndIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3nEUWlvcGmkaYTpc44hd2ZiaIXtZY4hW06EN{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFI1Njd5NUGg{txONg>? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzOFI2QS9pPmPBUmdGWjxxYU6=
T47D NIG0[WtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoK1TY5pcWKrdHnvckBw\iCqdX3hckBVPDeGIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTCyOE45Pzh|IN88UU4> MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzOFI2QS9pPmPBUmdGWjxxYU6=
NCI-H2029 MmPOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4XpWmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFI6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB{NT63PVY4KM7:TT6= M3P3[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFM1OjV7Lze+V2FPT0WUPD;hQi=>
NB6 MknTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYHJcohq[mm2aX;uJI9nKGi3bXHuJG5DPiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iMkWuPFc3PyEQvF2u M{HFSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFM1OjV7Lze+V2FPT0WUPD;hQi=>
BHT-101 MlXPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH7PNYFKdmirYnn0bY9vKG:oIHj1cYFvKEKKVD2xNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDJ4Lk[0OFMh|ryPLh?= NX7Ze3NDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzR{NUmvK|5USU6JRWK8M4E,
TK10 MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUnJcohq[mm2aX;uJI9nKGi3bXHuJHRMOTBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IEK2Mlg1QTVizszNMi=> NETmd5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{PDJ3OT:nQnNCVkeHUkyvZV4>
NCI-H2405 NGDSeGtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{jNVGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyOFA2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB{OT6wPFk2KM7:TT6= MlzPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|QzPTlxJ{7TRW5ITVJ:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
ppJAK1 / ppJAK2 / JAK1 / JAK2 ; 

PubMed: 26131691     


HDLM-2 cells treated with the indicated concentrations of methotrexate and aminopterin and blotted to show levels of total JAK1 (tJAK1), dual phosphorylated JAK1 (ppJAK1), total JAK2 (tJAK2), dual phosphorylated JAK2 (ppJAK2) and ß-actin shown as a loading control. Levels of ppJAK1 and ppJAK2 are reduced at high drug concentrations.

pSTAT1 / pSTAT3 / pSTAT5 / STAT1 / STAT3 / STAT5; 

PubMed: 26131691     


D) HDLM-2 cells treated with the indicated concentrations of methotrexate and aminopterin and blotted to show levels of total STAT1 (tSTAT1), phosphorylated STAT1 (pSTAT1), total STAT3 (tSTAT3), phosphorylated STAT3 (pSTAT3), total STAT5 (tSTAT5), phosphorylated STAT5 (pSTAT5) and β-actin shown as a loading control. Levels of pSTAT1 and pSTAT5 are reduced at most drug concentrations while levels of pSTAT3 appear to be unaffected.

AKT / p-AKT / mTOR / p-mTOR / Beclin 1 / HMGB1 ; 

PubMed: 26702616     


After the cells were exposed to 0.1 μM MTX for the indicated times, the cell lysates were subjected to Western blotting with specific antibodies. The results are representative of three independent experiments. β-actin was used as a loading control.

26131691 26702616
体内研究 在小鼠体内,Methotrexate增加脾细胞中AICAR含量,升高了角叉菜胶发炎气泡的渗出液中腺苷浓度,并且显著抑制了发炎气泡中白血球的积累。在小鼠体内,Methotrexate介导的白血球累积的减少被注射腺苷脱氨酶(ADA)到气泡而部分逆转,被特定的腺苷A2受体拮抗剂,3,7-dimethyl-1-propargylxanthine (DMPX)完全逆转,但不会被腺苷A1受体拮抗剂,8-cyclopentyl-dipropylxanthine所影响。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度 (25°C)

体外 DMSO 90 mg/mL warmed (198.04 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 454.44
化学式

C20H22N8O5

CAS号 59-05-2
储存条件 粉状
溶于溶剂
别名 NCI-C04671, Amethopterin, WR19039

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04483466 Not yet recruiting Drug: Methotrexate|Drug: Placebo Investigate the Effect(s) of Methotrexate Treatment on Arthritis Disease Severity George Washington University July 1 2022 Phase 3
NCT03642795 Not yet recruiting Other: Questionnaire Rheumatoid Polyarthritis Centre Hospitalier Universitaire de Nīmes October 2021 --
NCT04668768 Recruiting Drug: Glucarpidase Lymphoma Fox Chase Cancer Center April 16 2021 Phase 2
NCT04205734 Recruiting Diagnostic Test: MTX Assessment IBD Boston Children''s Hospital January 30 2021 --

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在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID