AZD1480

For research use only. Not for use in humans.

目录号:S2162

AZD1480 Chemical Structure

CAS No. 935666-88-9

AZD1480是一种新型,ATP竞争性的JAK2抑制剂,无细胞试验中IC50为0.26 nM,选择性作用于JAK3和Tyk2,对JAK1的作用较弱。Phase 1。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1071.19 现货
RMB 819.48 现货
RMB 4671.71 现货
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客户使用Selleck生产的AZD1480发表文献87篇:

产品安全说明书

JAK抑制剂选择性比较

生物活性

产品描述 AZD1480是一种新型,ATP竞争性的JAK2抑制剂,无细胞试验中IC50为0.26 nM,选择性作用于JAK3和Tyk2,对JAK1的作用较弱。Phase 1。
特性 AZD1480为治疗多发性骨髓瘤的潜在新型治疗剂。
靶点
JAK2 [1]
(Cell-free assay)
0.26 nM
体外研究

5μM AZD1480诱导细胞周期停在G2/M期,且通过抑制Aurora激酶而诱导细胞死亡。[1]AZD1480是JAK2的有效抑制剂,作用于人类多发性骨髓瘤细胞,可以抑制生长,存活,FGFR3 和 STAT3信号,及下游靶点,包括 Cyclin D2。在低微摩尔浓度时,AZD1480抑制细胞增殖和诱导骨髓瘤细胞系凋亡。[2]AZD1480 作用于人和鼠神经胶质瘤细胞,有效抑制组成型和诱导型JAK1, JAK2, 及STAT-3的磷酸化作用 ,结果导致细胞增殖降低,且诱导凋亡。[3]AZD1480是有效的ATP竞争性的JAK1/2激酶小分子抑制剂,可抑制STAT3磷酸化和肿瘤生长,这种抑制存在STAT3依赖性。AZD1480通过影响肿瘤的微环境而抑制肿瘤血管生成和局部转移。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SW620 MkjNSpVv[3Srb36gRZN{[Xl? MUS1JO69VQ>? NV;wdldyPDhiaB?= M4TocmROW09? NW\wUYtz[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o Mo\CQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NUS5O|QoRjJ3OUW0PVc1RC:jPh?=
LoVo  MV3GeY5kfGmxbjDBd5NigQ>? NHjTXo02KM7:TR?= MUW0PEBp MWLEUXNQ NFrUe5NjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> NF7jWXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm1OFk4PCd-MkW5OVQ6PzR:L3G+
HN5 M3\SVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzTfHc4OiCq M3jGdWVEPTB;Mz64NUDDuSBzLkm5JO69VQ>? Mn;EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MUCwNVAoRjJ3OEGwNFExRC:jPh?=
Cal33 NIPvfYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYe3NkBp NFLDUXpGSzVyPUOuN|chyrFiMD63OUDPxE1? M4Pkc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEGwNFExLz5{NUixNFAyODxxYU6=
UM-22B MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXT1c|REPzJiaB?= NEnBR4dGSzVyPUKuOlYhyrFiMD6yOEDPxE1? MmDUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MUCwNVAoRjJ3OEGwNFExRC:jPh?=
686LN NUPiXopKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7vRlI4OiCq MXnFR|UxRTJwMEWgxtEhOS5|MzFOwG0> M2nrZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEGwNFExLz5{NUixNFAyODxxYU6=
UM SCC-1 MonTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33yWFczKGh? Ml;3SWM2OD1zLk[3JOKyKDBwNEKg{txO NEfvOmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUixNFAyOCd-MkW4NVAxOTB:L3G+
UM-22A Mn\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LiTlczKGh? MUfFR|UxRTFwM{KgxtEhOC5|OTFOwG0> NGrDZnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUixNFAyOCd-MkW4NVAxOTB:L3G+
OSC19 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYO3NkBp NXPrTG5pTUN3ME2xMlI3KMLzIECuNlAh|ryP MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPThzMECxNEc,OjV6MUCwNVA9N2F-
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MOVCAR-5009 MkLkSpVv[3Srb36gRZN{[Xl? NIX1PZYxNjB3LUGwJO69VQ>? M4iyXlI1KGh? MYfEUXNQyqB? MmKydoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO= Mni4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NE[wNVUoRjJ3NkS2NFE2RC:jPh?=
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OVCAR-5 M3vQ[mNmdGxiVnnhZoltcXS7IFHzd4F6 NUHsOVNJOC5yNT2xNEDPxE1? MYS3NkBp MUPEUXNQ NHHWUW9z\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> NI\ne2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[0OlAyPSd-MkW2OFYxOTV:L3G+
OVCAR-8  MXfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWiwMlA2NTFyIN88US=> NYXTe4xkPzJiaB?= MXnEUXNQ MnTydoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2= MoL0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NE[wNVUoRjJ3NkS2NFE2RC:jPh?=
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OVCAR-8  M2j4eWFxd3C2b4Ppd{BCe3OjeR?= M3jVfVAvPS9zL{Wg{txO M{fMPFQ5KGh? M4PaOmROW09? NWW5bnBRcW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=> MnfCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NE[wNVUoRjJ3NkS2NFE2RC:jPh?=
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DU145  M4LLbGZ2dmO2aX;uJGF{e2G7 MV[wMVIxOCCwTR?= NUi2bJRCOSCqwrC= NHvDdXl{fXCycnXzd4V{KEmOLU[tZYN1cX[jdHXkJHN1[XR|IHHu[EBGWktzL{Kgd4lodmGuaX7n MmL5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFIoRjJ2NUe3PVQzRC:jPh?=
DU145  NWXncph1TnWwY4Tpc44hSXO|YYm= Mn3FPFAxKG6P M1u3clczKGh? Mn;Xd5VxeHKnc4Pld{BKVC14LXnu[JVk\WRibXnndoF1d3K7 M4PhNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUe3PVQzLz5{NEW3O|k1OjxxYU6=
CWR22Rv1 NImzS2NHfW6ldHnvckBCe3OjeR?= MojGPFAxKG6P MlPRO|IhcA>? NYDBclhbe3WycILld5NmeyCLTD22MYlv\HWlZXSgcYloemG2b4L5 MnHDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFIoRjJ2NUe3PVQzRC:jPh?=
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GLC4 M2Hxb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvLNXBQUUN3ME2xMlc6KM7:TR?= NIjVZWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG1PFcxOSd-MkSxOVg4ODF:L3G+
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L-428 MmmzRZBweHSxc3nzJGF{e2G7 M4\NeVEwPSEQvF2= MUC3NwKBkWh? NVrzWHl7TE2VTx?= MknkbY5lfWOnczDhdI9xfG:|aYO= NHLQdW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkiyPVA6PCd-MkK4NlkxQTR:L3G+
KM-H2 MX\BdI9xfG:|aYOgRZN{[Xl? M{fHT|EwPSEQvF2= NX3UV4ZTPzMkgJno MnjISG1UVw>? NWLyUHdRcW6mdXPld{BieG:ydH;zbZM> NWGz[ng1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4NlkxQTRpPkKyPFI6ODl2PD;hQi=>
L-540 M{PBRmFxd3C2b4Ppd{BCe3OjeR?= NUPMenhIOS93IN88US=> M1G4VFcz6oDLaB?= M1zy[WROW09? NWrF[pljcW6mdXPld{BieG:ydH;zbZM> MlzmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MkmwPVQoRjJ{OEK5NFk1RC:jPh?=
U251-MG M1LTUmZ2dmO2aX;uJGF{e2G7 MXSxJOK2VQ>? MVmwMVE3KGh? NF\NZnNqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? M4K5dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MEK3OlkyLz5{MkCyO|Y6OTxxYU6=
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4C8 M3TLO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDKNU8yOCEEtV2= Ml;KNlQwPDhxN{KgbC=> M2fCOYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO NEi5VnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkCyO|Y6OSd-MkKwNlc3QTF:L3G+
U266 M2qwNmFxd3C2b4Ppd{BCe3OjeR?= NVPGXYVrOC53LUKg{txO MYC0PE84OiCq MUHpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NGXsNlk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUG2OFUyPyd-MkGxOlQ2OTd:L3G+
Kms.11 Mn64RZBweHSxc3nzJGF{e2G7 MmHkNE42NTJizszN MUm0PE84OiCq M4LUe4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M1T0bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMU[0OVE4Lz5{MUG2OFUyPzxxYU6=
8226 NXjGWWh5SXCxcITvd4l{KEG|c3H5 NIewWIoxNjVvMjFOwG0> Moe1OFgwPzJiaB?= Mmq0bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTF4NEWxO{c,OjFzNkS1NVc9N2F-
SET2 M4rlfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGjIPYQ1QCCqcoO= M2\zTWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJHNGXDJiY3XscJMh\XiycnXzd4lv\yCMYXuyJHY3OTeIIH31eIFvfCCjZoTldkA1QCCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwJF0hOC5yMU[g{txONg>? NWi1ZWQ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGxN|gzPDZpPkKxNVM5OjR4PD;hQi=>
SET2 MlXDSpVv[3Srb36gZZN{[Xl? NVvpfVc{OSCqch?= NY\XVXcxUW6qaXLpeIlwdiCxZjDTeIF1OyCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hW0WWMjDj[YxteyCjZoTldkAyKGi{IHL5JHdme3Sncn6gZoxwfHSrbnesJGlEPTBiPTCwMlAzOyEQvF2u NG\DRWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUGzPFI1Pid-MkGxN|gzPDZ:L3G+
SET2 MoexSpVv[3Srb36gZZN{[Xl? NF\ne|QyKGi{ NFjjUY5KdmirYnn0bY9vKG:oIGP0ZZQ2KHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBUTVR{IHPlcIx{KGGodHXyJFEhcHJiYomgW4V{fGW{bjDicI91fGmwZzygTWM2OCB;IECuNFI2KM7:TT6= NX\yVYt7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGxN|gzPDZpPkKxNVM5OjR4PD;hQi=>
HEL Mln5SpVv[3Srb36gZZN{[Xl? M4\qflEhcHJ? NXLZZZUyUW6qaXLpeIlwdiCxZjDTeIF1PSCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hUEWOIHPlcIx{KGGodHXyJFEhcHJiYomgW4V{fGW{bjDicI91fGmwZzygTWM2OCB;IECuNFQyKM7:TT6= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTF|OEK0Okc,OjFzM{iyOFY9N2F-
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HEL MlzCSpVv[3Srb36gZZN{[Xl? M1\V[lEhcHJ? Mn3XTY5pcWKrdHnvckBw\iCVdHH0N{BxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gTGVNKGOnbHzzJIFnfGW{IEGgbJIh[nliV3XzeIVzdiCkbH;0eIlv\yxiSVO1NEA:KDBwMEig{txONg>? NHi2d2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUGzPFI1Pid-MkGxN|gzPDZ:L3G+
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HEL NUXLZlRUTnWwY4Tpc44h[XO|YYm= NFvB[XMxNjNidV2= M4LlbFMxKHSxIE[wJI1qdnN? NGXscWFKdmirYnn0bY9vKG:oIGP0ZZQ{KHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBJTUxiY3XscJMh[XRiMD6zJJVOKGGodHXyJFMxKHSxIE[wJI1qdnNiYomgW4V{fGW{bjDicI91fGmwZx?= NHPsdGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUGzPFI1Pid-MkGxN|gzPDZ:L3G+
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BT-37 NWO1PWFseUiWUzDhd5NigQ>? MVHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN? NIXhOpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 M2fqWJFJXFNiYYPzZZk> MkXwdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6ELVXCZ|Eh[2WubIO= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Saos-2 NVj6bVBneUiWUzDhd5NigQ>? M13GNJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO= NGLvXXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-SH M1\tUpFJXFNiYYPzZZk> NH7FcmVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1UUCClZXzsdy=> NEnu[oE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB1643 MmTYdWhVWyCjc4PhfS=> NEHEfmZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz M1fwUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-12 MVrxTHRUKGG|c3H5 MXvxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN? MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 MoHkdWhVWyCjc4PhfS=> NEfyPYRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz NF7KWlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
RD MWTxTHRUKGG|c3H5 MYLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) M1jYS5FJXFNiYYPzZZk> MkC3dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy| NF7XfFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 Mlv4dWhVWyCjc4PhfS=> NWLGU|R{eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoOFEh[2WubIO= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-STAT3 / STAT3 / p-JAK2 / JAK2 ; 

PubMed: 22027691     


Cells were treated with AZD1480 for the indicated times, lysed and immunoblotted with the indicated antibodies. 

p-STAT1 / STAT1 / p-STAT5 / STAT5 / p-STAT6 / STAT6 ; 

PubMed: 22829094     


Western blot assay of the four HL cell lines treated with increasing doses of AZD1480 (0.1–5 μM) for 72 h. 

p-ERK / ERK / p-p38 / p38 / SOCS3 / p-SHP2 / SHP2 ; 

PubMed: 22829094     


Representative western blot assay showing increased levels of ERK, p38 and SHP-2 phosphorylation in HD-LM2 and L-428, after treatment for 72 h with increasing doses of AZD1480 (0.1-5 μM). In contrast, L-540 showed a dose-dependent inhibition of ERK and p38 activation without increased SHP-2 phosphorylation. SOCS-3 levels decreased in all the cell lines.

22027691 22829094
Immunofluorescence
pSTAT5; 

PubMed: 30140255     


HepG2 cells were incubated in the presence of Pro-Gly (0.5 mM) and/or AZD1480 (1 μM) for 6 h and phospho-STAT5 translocation to nuclei was detected by ICC. Scale bar, 10 μm. The IP and ICC experiments were conducted independently for 3 times, with 3 replicates each time.

30140255
Growth inhibition assay
Cell proliferation ; 

PubMed: 22027691     


Cells were treated with AZD1480 for the indicated times, and the WST-1 cell proliferation assay performed. The 48 and 72 h time points were statistically significant. Data represent mean ± SD, replicates of three (**, p<0.001; ANOVA). 

Cell viability; 

PubMed: 25855603     


IL-3-independent Ba/F3 cells were treated with increasing concentrations of the JAK inhibitor AZD1480 showing submicromolar inhibition of proliferation.

22027691 25855603
体内研究 AZD1480作用于人类实体瘤模型和多发性骨髓瘤模型,抑制 STAT3磷酸化。[1]在体内, AZD1480抑制皮下移植瘤的生长,且通过抑制STAT3活性提高携带颅内恶性胶质瘤(GBM)的鼠寿命,说明AZD1480抑制JAK/STAT3通路的药理学可以用于研究治疗携带颅内恶性胶质瘤的患者。[3]AZD1480抑制骨髓细胞的肺浸润和肺转移瘤。AZD1480作用于人类移植瘤模型降低血管生成和代谢。[4]AZD1480抑制含有STAT活性的人类实体瘤的生长。[5]

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:[5]
- 合并

激酶实验:

在有buffer(包括50 mM HEPES pH 为7.3, 1 mM DTT, 0.01% Tween-20, 50 µg/ml BSA,及10 mM MgCl2)的条件下,使用重组Jak1, Jak2, 或Jak3进行AZD1480抑制效果研究。在昆虫细胞中,Jak3酶表达为氮端GST融合蛋白,且通过谷胱甘肽亲和及尺寸排除色谱来纯化Jak3酶。加入AZD1480 (10点剂量反应, 重复三次, 8.3 µM 到0.3 nM ),使用1.5 µM 肽底物(Jak1:FITC-C6-KKHTDDGYMPMSPGVA-NH2, Jak2和Jak3: FAM-SRCtide),及各自ATP Km (Jak1: 55 µM, Jak2: 15 µM, Jak3: 3 µM),ATP浓度为5 mM,进行酶实验。分离磷酸化和未磷酸化的肽段,使用Caliper LC3000系统计算抑制百分率。
细胞实验:[4]
- 合并
  • Cell lines: Renca或786-O细胞,鼠内皮细胞和脾CD11b+/c−骨髓细胞, HUVECs
  • Concentrations: 1 μM
  • Incubation Time: 48或24小时
  • Method: Renca或786-O细胞悬浮在含5%FBS的DMEM培养基中,按每孔5×103个细胞接种在96孔板上,使细胞粘附,实验组用AZD1480,对照组用DMSO,处理48小时。通过MTS实验测定细胞活力。使用Mikrotek Laborsysteme在490nm处测定吸光值。鼠内皮细胞和脾CD11b+/c− 骨髓细胞从携带肿瘤的鼠中富集得到,培养在含5% FBS的RPMI-1640培养基上。HUVECs 培养在胶原1包被的含完全培养基的板上。用DMSO和不同剂量AZD1480处理所有细胞,持续24小时。手动计算细胞数而测定细胞活力。所有实验重复三次。
    (Only for Reference)
动物实验:[4]
- 合并
  • Animal Models: 雌性BALB/c和无胸腺鼠(NCR− nu/nu) (7-8周大)
  • Dosages: 每天一次,剂量为50 mg/kg;或者每天两次,剂量为30 mg/kg
  • Administration: 口服饲喂
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 69 mg/mL warmed (197.83 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):
30% PEG400+0.5% Tween80+5% propylene glycol
5 mg/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 348.77
化学式

C14H14ClFN8

CAS号 935666-88-9
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、MSDS / 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、MSDS / 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
NCT01219543 Terminated Drug: AZD1480 Daily|Drug: AZD1480 BID Solid Tumour|Advanced Solid Malignancies|Child-Pugh A to B7 Advanced Hepatocellular Carcinoma|EGFR and/or ROS Mutant NSCLC|Lung Metastasis Carcinoma|Gastric Cancer AstraZeneca November 2010 Phase 1
NCT01112397 Terminated Drug: AZD1480 Solid Malignancies AstraZeneca April 2010 Phase 1

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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

如果有其他问题,请给我们留言。

  • * 必填项

JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID