Letrozole (CGS 20267)

For research use only. Not for use in humans.

目录号:S1235 中文名称:来曲唑

Letrozole (CGS 20267) Chemical Structure

CAS No. 112809-51-5

Letrozole (CGS 20267) 是第三代aromatase抑制剂,无细胞试验中IC50为0.07-20 nM。在临床研究中,对17α-OH progesterone、TSH、促黄体激素、促卵泡激素或雄烯二酮的血浆浓度没有作用,不影响正常的尿电解质排泄或甲状腺功能。Letrozole 可诱导自噬。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 3930.28 现货
RMB 814.34 现货
RMB 1383.01 现货
RMB 2350.53 现货
RMB 3866.75 现货
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客户使用Selleck生产的Letrozole (CGS 20267)发表文献23篇:

产品安全说明书

Aromatase抑制剂选择性比较

生物活性

产品描述 Letrozole (CGS 20267) 是第三代aromatase抑制剂,无细胞试验中IC50为0.07-20 nM。在临床研究中,对17α-OH progesterone、TSH、促黄体激素、促卵泡激素或雄烯二酮的血浆浓度没有作用,不影响正常的尿电解质排泄或甲状腺功能。Letrozole 可诱导自噬。
靶点
Aromatase [1]
(Cell-free assay)
0.07 nM-20 nM
体外研究

Letrozole有效抑制不同来源的芳香酶,包括人胎盘微粒体,人乳腺癌颗粒部分,大鼠卵巢微粒体,转染芳香酶的MCF-7细胞(MCF-7Ca),JEG-3绒膜癌细胞,CHO细胞,仓鼠卵巢组织,人乳腺癌颗粒部分,IC50分别是11, 2, 7, 0.07, 0.07, 1.4, 20和 0.8 nM。在非细胞系统中,letrozole 的IC50是1-13 nM。[1]Letrozole在LH诱导的仓鼠卵巢组织中抑制雌二醇产生,IC50 是0.02 μM,达到350 μM浓度时,不显著影响孕酮的产生。在ACTH诱导的大鼠肾组织中,抑制醛甾酮的产生,IC50 是210 μM. [2] Letrozole以剂量依赖的方式抑制MCF-7乳腺癌细胞的生长,IC50是1 nM。在低浓度下(0.1 nM)抑制作用依然可以观测到。letrozole 处理MCF-12A不影响生长,即使letrozole 浓度达到 (100 nM)或者延长培养时间。Letrozole (10 nM) 显著抑制4-雄甾烯-3,17-二酮(100 nM) 或者睾酮 (100 nM) 对MCF-7在细胞增殖方面的激活作用。联合使用17-β-雌二醇和letrozole (10 nM)降低由雌二醇诱导的MMP-2和MMP-9的活化作用。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
JEG3 M2HnTWZ2dmO2aX;uJIF{e2G7 NFHmbFRKdmirYnn0bY9vKG:oIHHyc41ifGG|ZTDhZ5Rqfmm2eTDpckBpfW2jbjDKSWc{KGOnbHzzMEBKSzVyPUCuNFAxQDoQvF2= NH\Edow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEW5NFI4Oid-MUi1PVAzPzJ:L3G+
JEG3 MlPHSpVv[3Srb36gZZN{[Xl? NILORmJKdmirYnn0bY9vKG:oIHHyc41ifGG|ZTDpckBpfW2jbjDKSWc{KGOnbHzzJIJ6KHOlaX70bYxt[XSrb36gd5Bm[3S{b33leJJ6NCCLQ{WwQVAvODByOEpOwG0> M3XQdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMUS4OVY1Lz5{MEG0PFU3PDxxYU6=
MDA-MB-435 NIPNN21Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGfDWG01QCCqcoO= M3ftV2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj20N|Uh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEeLNUC9NE4xPjgQvF2= MnfCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB7NUC4PVgoRjJyOUWwPFk5RC:jPh?=
IGROV1 MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWH1XId5PDhiaILz NEXTOFRIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBKT1KRVkGgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KHO3bH\vdohw\GGvaX7lJGIh[XO|YYmsJGdKPTB;MD6wPVXPxE1? MnizQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB7NUC4PVgoRjJyOUWwPFk5RC:jPh?=
MDA-MB-231 MlG2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVvxcHBXPDhiaILz NUjTPJg3T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVI{OWOnbHzzJIFnfGW{IES4JIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F6NCCJSUWwQVAvOTYQvF2= M4Hkd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOUWwPFk5Lz5{MEm1NFg6QDxxYU6=
T47D M1;SR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn;POFghcHK| M1Hr[Wdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJHQ1P0RiY3XscJMh[W[2ZYKgOFghcHK|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[XluIFfJOVA:OC52NN88US=> NI\ZcI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEm1NFg6QCd-MkC5OVA5QTh:L3G+
MCF7 NVzhPXhIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXPoemxTPDhiaILz NUixWZNvT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVUOINzDj[YxteyCjZoTldkA1QCCqcoOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeTygS2k2OD1yLkhOwG0> NUL5S2gxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC5OVA5QThpPkKwPVUxQDl6PD;hQi=>
OVCAR4 NVPXb2RKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVy0PEBpenN? M3ToUWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG9XS0GUNDDj[YxteyCjZoTldkA1QCCqcoOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeTygS2k2OD1yLki4{txO NUXNXlRTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC5OVA5QThpPkKwPVUxQDl6PD;hQi=>
BT549 M1[0fWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlzkOFghcHK| Mni3S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gRnQ2PDliY3XscJMh[W[2ZYKgOFghcHK|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[XluIFfJOVA:OC56Od88US=> M37ocFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOUWwPFk5Lz5{MEm1NFg6QDxxYU6=
SKOV3 MneyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXu0PEBpenN? MkjWS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gV2tQXjNiY3XscJMh[W[2ZYKgOFghcHK|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[XluIFfJOVA:OS5yOd88US=> NX3ZXIJqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC5OVA5QThpPkKwPVUxQDl6PD;hQi=>
NCI/ADR-RES Mn\IS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH3sdm81QCCqcoO= MlyxS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUmNKN0GGUj3SSXMh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEeLNUC9NU4yPs7:TR?= MofGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB7NUC4PVgoRjJyOUWwPFk5RC:jPh?=
MDA-N NGnzfIJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIrkOpY1QCCqcoO= NFPCbFRIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTjDj[YxteyCjZoTldkA1QCCqcoOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeTygS2k2OD1zLk[x{txO NUXUT21zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC5OVA5QThpPkKwPVUxQDl6PD;hQi=>
OVCAR5 M1r5XWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NW\UUHl6PDhiaILz NYrEdnhmT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWK1JINmdGy|IHHmeIVzKDR6IHjyd{BjgSC|dXzmc5Jpd2SjbXnu[UBDKGG|c3H5MEBIUTVyPUGuOlLPxE1? M13XPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOUWwPFk5Lz5{MEm1NFg6QDxxYU6=
Hs 578T NF7uTYtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHi5doc1QCCqcoO= Mmm3S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTJMhPTd6VDDj[YxteyCjZoTldkA1QCCqcoOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeTygS2k2OD1{LkG3{txO M1XlSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOUWwPFk5Lz5{MEm1NFg6QDxxYU6=
OVCAR8 MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWK0PEBpenN? MXHHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDPWmNCWjhiY3XscJMh[W[2ZYKgOFghcHK|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[XluIFfJOVA:PC53zszN MoHJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB7NUC4PVgoRjJyOUWwPFk5RC:jPh?=
OVCAR3 M4PjW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEfHenU1QCCqcoO= MlK1S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gU3ZESVJ|IHPlcIx{KGGodHXyJFQ5KGi{czDifUB{fWyob4Loc4RidWmwZTDCJIF{e2G7LDDHTVUxRTVwOEhOwG0> NUSyXlJkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC5OVA5QThpPkKwPVUxQDl6PD;hQi=>
MCF7a M3;sNGN6fG:2b4jpZ4l1gSCjc4PhfS=> MXuxNEBl[Xm| MlfWR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHP2FiY3XscJMh\XiycnXzd4lv\yCWZYStc4ZnNTOkZYThTHNFOS2Dcn;tJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gWHNVNXO2aX31cIF1\WRiY3XscEBxem:uaX\ldoF1cW:wIH3lZZN2emWmIHHmeIVzKDFyIHThfZMtKEWFNUC9NE4xODByMEVOwG0> NVm3enRuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5OVExPzRpPkKyPVUyODd2PD;hQi=>
V79MZh MYDGeY5kfGmxbjDhd5NigQ>? NY\ieo5yUW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIzKGW6cILld5Nm\CCrbjDoZY1{fGW{IG[3PW1bcCClZXzsd{B2e2mwZzDbNUwzNTOKXT2xNU1l\W:6eT3jc5J1cWOxc4Tldo9v\SCjczDzeYJ{fHKjdHWsJGlEPTB;MT60Nu69VQ>? NYPKdmpYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyPFE5OTJpPkKzNlgyQDF{PD;hQi=>
V79MZh Mon0SpVv[3Srb36gZZN{[Xl? M4rLfGlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNUBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXogh[2WubIOgeZNqdmdiW{GsNk0{UF1vMUGt[IVwgHlvY3;yeIlkd3O2ZYLvcoUh[XNic4Xid5Rz[XSnLDDJR|UxRTJwNkNOwG0> NEHZdmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K4NVgyOid-MkOyPFE5OTJ:L3G+
H295R NH3TXFJHfW6ldHnvckBie3OjeR?= NF\hWWM2KHWP NEPwU5YzPCCqcoO= NX;wOY5WUW6qaXLpeIlwdiCxZjDDXXAyQSCrbjDoeY1idiCKMkm1VkBk\WyuczD1d4lv\yCdMXLleIEuO0hqTjndMYFv\HKxc4StOE1mdmVvMzyxO{1lcW:wZTDheEA2KHWPIHHmeIVzKDJ2IHjyd{BjgSC2cnn0bYF1\WRid3H0[ZIhemWuZXHz[UBie3OjeR?= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB{NUC2PUc,OjRyMkWwOlk9N2F-
MCF7 NH\GbFFEgXSxdH;4bYNqfHliYYPzZZk> NEPhXWs4OiCqcoO= MmTuR5l1d3SxeHnjbZR6KGGpYXnud5Qh\XO2cn;n[Y4u\GWyZX7k[Y51KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlAxP87:TR?= M{Wx[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{S1OFgyLz5{NEO0OVQ5OTxxYU6=
MCF7 NWjWeWVQS3m2b4TvfIlkcXS7IHHzd4F6 NE\iRoUzPCC2bzC5OkBpenN? NGrZWo1EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFI1KHSxIEm2JIhzeyxiSVO1NF0xNjB{zszN MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN2NUS4NUc,OjR|NEW0PFE9N2F-
JEG-3 NXLBc5gxTnWwY4Tpc44h[XO|YYm= MoGxTY5pcWKrdHnvckBw\iCjcn;tZZRie2ViKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gTmVINTNiY3XscJMtKEmFNUC9NE4xODB6Od88US=> M{DtVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUmyPFgxLz5{NUm5Nlg5ODxxYU6=
insect cells M{fn[WZ2dmO2aX;uJIF{e2G7 MnTHN|AhdWmwcx?= MYfJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKEO\UEG5JIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDpcpNm[3RiY3XscJMhfXOrbnegUWZEKGG|IIP1ZpN1emG2ZTDt[YF{fXKnZDDh[pRmeiB|MDDtbY5{KGK7IH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME2wMlAxPTQQvF2= NV[yPWhzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke2OFc{PjdpPkK3OlQ4OzZ5PD;hQi=>
T47D MlWzSpVv[3Srb36gZZN{[Xl? MofMNlQhcHK| MoKyTY5pcWKrdHnvckBw\iCjcn;tZZRie2ViYXP0bZZqfHliaX6gbJVu[W5iVES3SEBk\WyuczDh[pRmeiB{NDDodpMtKEmFNUC9NlkvPc7:TR?= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzd5MEezOUc,Ojd5N{C3N|U9N2F-
T47D MWPGeY5kfGmxbjDhd5NigQ>? NHTTXngzPCCqcoO= NYLIUJJwUW6qaXLpeIlwdiCxZjDhdo9u[XSjc3WgZYN1cX[rdImgbY4hcHWvYX6gWFQ4TCClZXzsd{Bi\nSncjCyOEBpenNuIFnDOVA:OjlwNd88US=> MoHIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2MkewNVcoRjJ6NEK3NFE4RC:jPh?=
MCF7 M3y5R2N6fG:2b4jpZ4l1gSCjc4PhfS=> NXntTWVrPDhiaILz NGPORY9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9OE44O87:TR?= M1PPO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MkCyOFA2Lz5{OUKwNlQxPTxxYU6=
MCF7 NX36TJJRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2HSTlczKGi{cx?= M{j6OGdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1ETjdiY3XscJMhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgZ4VtdCClb4XueIlv\yCkYYPl[EBu\XSqb3SsJGdKPTB;ND6x{txO NYHHRYs5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C4NlI4OTNpPkOwPFIzPzF|PD;hQi=>
MDA-MB-231 MmHZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVy3NkBpenN? M3jlcmdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgbY5kfWKjdHXkJIZweiB5MjDodpMh[nliY3XscEBkd3WwdHnu[{Bj[XOnZDDt[ZRpd2RuIFfJOVA:OTEQvF2= NV3ySXVrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C4NlI4OTNpPkOwPFIzPzF|PD;hQi=>
insect cells NHj4T2pHfW6ldHnvckBie3OjeR?= MULJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKGG{b33heIF{\SCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhcW6|ZXP0JINmdGy|IIXzbY5oKE9vYnXufpltKG[udX;y[ZNk\WmwIHLlcpp6dCCnc4TldkBieyC|dXLzeJJifGViaX6gdJJme2WwY3Wgc4YhVkGGUFig[4Vv\XKjdHnu[{B{gXO2ZX2gZpkh\my3b4Lld4NmdmOnIHLhd4VlKGGwYXz5d4l{NCCLQ{WwQVAvODBzOd88US=> M3frN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNEG2O|M5Lz5|MUSxOlc{QDxxYU6=
MCF-7aro MXLGeY5kfGmxbjDhd5NigQ>? NWT6TZQ3OSCqch?= NFu1S5FKdmirYnn0bY9vKG:oIHHyc41ifGG|ZTDpckBpfW2jbjDNR2YuP2G{bzDj[YxteyC3c3nu[{BcOWKndHGtN2heKGGwZILvd5RmdmWmaX;u[UBieyC|dXLzeJJifGViaX7jeYJifGWmIH\vdkAyKGi{IHL5JIxqeXWrZDDzZ4lvfGmubHH0bY9vKGOxdX70bY5oKG2ndHjv[EwhUUN3ME2wMlAxOToQvF2= M2Dn[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzN{OyNlUzLz5|MUezNlI2OjxxYU6=
insect cells NG\DfnVHfW6ldHnvckBie3OjeR?= MYezNEBucW6| NWXDWoR2UW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDhdo9u[XSjc3Wg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|IHnu[oVkfGWmIHnud4VkfCClZXzsd{B2e2mwZzDPMYJmdnq7bH\seY9z\XOlZXnuJIJmdnq7bDDld5RmeiCjczDzeYJ{fHKjdHWgZYZ1\XJiM{CgcYlveyxiSVO1NF0xNjByMUJOwG0> NITDR3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPDR2Lze+R4hGVUKOPD;hQi=>

... Click to View More Cell Line Experimental Data

体内研究 在体内实验中, Letrozole抑制芳香酶活性,口服ED50 是1-3 微克/毫克。[2] Letrozole具有抗内分泌效果。在未成年大鼠体内,Letrozole抑制雄烯二酮引起的子宫肥大,ED50 为1-3 微克/千克。在成年雌性大鼠体内,Letrozole (0.3-1 毫克/千克 每天 口服,14 天)完全打断卵巢周期,并降低子宫重量和血清雌二醇(E2)浓度,使其与切除卵巢后的水平相同。[1] Letrozole诱导剂量依赖的雌激素依赖的抑制9,10-二甲苯-a-蒽 (DMBA)诱导的雌性大鼠的肿瘤。Letrozole 的ED50是10-30 微克/千克/天,完全抑制的剂量是10微克/天。[4]

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)

激酶实验:

[6]

- 合并

人类胎盘芳香酶活性:

反应在37℃条件下,总体积为1 mL的体系中进行。孵育的混合物包含11 nM [4- 14C] 雄甾烯-3, 17-二酮([4- 14C]A),24 mM NADPH (焦磷酸钠盐III型),适当浓度的化合物,120 μg微粒体蛋白。(4- 14C)A用含有1.7% 溶解,溶于的0.05 M 磷酸钾缓冲液 (pH 7.4)溶解,乙醇终浓度不超过0.02%。加入酶触发反应,20分钟后加入7倍体积乙酸乙酯终止反应。混合物震荡,600g离心5分钟。用7倍体积的乙酸乙酯重新提起,混合两次所得样品,Evapo-Mix蒸干。用这种方法,99%的[4- 14C]的放射性能够保留。获得的残渣溶于150ul丙酮,取100ul做65分钟的薄层层析,用体积比为140:60的乙酸乙酯:异辛烷或者体积比为70:140:20(系统B)。用Berthold LB 2760定位放射性区域。放射性标记的雌二醇和孕酮通过与标准品比对来确认。硅胶结合的条带转移到10ml闪烁缓冲液中,用6880液体闪烁法系统计数。
细胞实验:

[3]

- 合并
  • Cell lines: 人类乳腺癌细胞 MCF-7
  • Concentrations: ~100 nM
  • Incubation Time: 1天
  • Method:

    细胞以5,000 到10,000个每孔的密度接种于24孔板上,第二天,加入不同浓度的Letrozole。孵育末期,细胞用胰酶消化,用Coulter particle计数器计数。


    (Only for Reference)
动物实验:

[5]

- 合并
  • Animal Models: 含有人类芳香化酶基因(MCF-7Ca)的人类乳腺癌异种移植MCF-7
  • Dosages: 20毫克/千克/天
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 57 mg/mL (199.78 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):
0.5% CMC Na
10mg/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 285.3
化学式

C17H11N5

CAS号 112809-51-5
储存条件 粉状
溶于溶剂
别名 N/A

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
NCT04714619 Recruiting Drug: CB-103 Advanced Breast Cancer MedSIR|Cellestia Biotech AG April 2021 Phase 2
NCT04735367 Not yet recruiting Drug: palbociclib plus letrozole Breast Cancer Pfizer February 1 2021 --
NCT04227327 Recruiting Drug: Abemaciclib|Drug: Aromatase Inhibitors Advanced Breast Cancer University of Milano Bicocca January 7 2020 Phase 2
NCT03870919 Recruiting Drug: Palbociclib|Other: locoregional treatment Breast Cancer Stage IV|Radiotherapy|Surgery UNICANCER|Pfizer October 23 2019 Not Applicable

技术支持

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

如果有其他问题,请给我们留言。

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Aromatase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID