AZD1480 化学構造
分子量: 348.77

高品質保証

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Quality Control & MSDS

製品説明

  • Compare JAK Inhibitors
    JAK製品生物活性の比較
  • 研究分野
  • AZD1480のメカニズム

製品の説明

生物活性

製品説明 AZD1480は、JAK1とJAK2の新しいATP競争的阻害剤で、IC50がそれぞれ 1.3 nM と 0.26 nMです。
ターゲット JAK2
IC50 0.26 nM [1]
In vitro試験 5μM AZD1480 induces G2/M arrest and cell death by inhibiting Aurora kinases. [1] AZD1480 is a potent JAK2 inhibitor that can suppress growth, survival, as well as FGFR3 and STAT3 signaling and downstream targets including Cyclin D2 in human multiple myeloma cells. At low micromolar concentrations, AZD1480 blocks cell proliferation and induces apoptosis of myeloma cell lines. [2]AZD1480 effectively blocks constitutive and stimulus-induced JAK1, JAK2, and STAT-3 phosphorylation in both human and murine glioma cells, and leads to a decrease in cell proliferation and induction of apoptosis. [3]AZD1480 is a potent, competitive small-molecule inhibitor of JAK1/2 kinase, and that it is capable of inhibiting STAT3 phosphorylation and tumor growth in a STAT3-dependent manner. AZD1480 inhibits tumor angiogenesis and metastasis in part by affecting the tumor microenvironment. [4]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
SW620 M4m4dGZ2dmO2aX;uJGF{e2G7 NWrp[GNxPSEQvF2= NXntR4ZwPDhiaB?= NIT1e4VFVVOR NFe0cmpjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc> MVKyOVk2PDl5NB?=
LoVo  NIPPUmJHfW6ldHnvckBCe3OjeR?= MYW1JO69VQ>? M4HmV|Q5KGh? MnHySG1UVw>? M1Hwb4Jtd2OtczDKRWszN1OWQWSzJJNq\26jbHnu[y=> MnrUNlU6PTR7N{S=
HN5 M1Ozdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVu1O3F6PzJiaB?= MoLsSWM2OD1|LkixJOKyKDFwOUmg{txO NULzRYdYOjV6MUCwNVA>
Cal33 MoG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHe5dI04OiCq NX;FfY9UTUN3ME2zMlM4KMLzIECuO|Uh|ryP M4jkW|I2QDFyMEGw
UM-22B NFPtU4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWO3NkBp Mlz5SWM2OD1{Lk[2JOKyKDBwMkSg{txO M3nnR|I2QDFyMEGw
686LN NEKxbJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{e2fFczKGh? M4S4bmVEPTB;Mj6wOUDDuSBzLkOzJO69VQ>? Mk\aNlU5OTByMUC=
UM SCC-1 NWTnT2hLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PKblczKGh? NXHtdZU1TUN3ME2xMlY4KMLzIECuOFIh|ryP NGLqVW8zPThzMECxNC=>
UM-22A NFfPdHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYK3NkBp M{XjbWVEPTB;MT6zNkDDuSByLkO5JO69VQ>? MYWyOVgyODBzMB?=
OSC19 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjjO|IhcA>? NF3EWndGSzVyPUGuNlYhyrFiMD6yNEDPxE1? NIXWfnIzPThzMECxNC=>
PCI-52 MnLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV:3NkBp NYjHVnBtTUN3ME2xMlAxKMLzIECuNFkh|ryP NW\vXGNyOjV6MUCwNVA>
PCI-15B NYHpcWZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvVO|IhcA>? NGHTXGxGSzVyPUCuPVkhyrFiMT63OEDPxE1? MnrDNlU5OTByMUC=
UMSCC-1 Mo\DSpVv[3Srb36gRZN{[Xl? MYCwMlAxODVvMT62JO69VQ>? NVm1eIJYOjRiaB?= MoHiZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mn63NlU5OTByMUC=
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TPC-1 Mlu2SpVv[3Srb36gRZN{[Xl? NUDUc5pEOSEEtV2= NVP6cHJtPzJiaB?= MmraSG1UVw>? NWfYbXpRcW6mdXPld{BIOSCkbH;jb4Fo\Q>? MUeyN|A2PjR7OR?=
MZ-CRC1  M{\0eGZ2dmO2aX;uJGF{e2G7 MUOxJOK2VQ>? NGX3Rng4OiCq Mk\uSG1UVw>? M1jmcYlv\HWlZYOgS|Eh[myxY3vh[4U> NGrMe3MzOzB3NkS5PS=>
TT  MoL2SpVv[3Srb36gRZN{[Xl? M1LoXlEhyrWP NIXFUWg4OiCq NXvqd3cyTE2VTx?= MkTXbY5lfWOnczDHNUBjdG:la3Hn[S=> MWmyN|A2PjR7OR?=
MZ-CRC1  M2TTVGFxd3C2b4Ppd{BCe3OjeR?= MYqxJOK2VQ>? NXPUXVBRPDhiaB?= MoLISG1UVw>? NV7WfZFMcW6mdXPld{BieG:ydH;zbZM> MnfMNlMxPTZ2OUm=
TT  M3nNb2Fxd3C2b4Ppd{BCe3OjeR?= NEGxeGkyKML3TR?= MXK0PEBp MoLQSG1UVw>? M{LtNolv\HWlZYOgZZBweHSxc3nz MYiyN|A2PjR7OR?=
HD-LM2 NVHWN2gyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jsXlcz6oDLaB?= MWLEUXNQ NFixdI5KSzVyPUeuPFQ1KM7:TR?= NIHpVI0zOjh{OUC5OC=>
L-428 NWL5XXZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWi3NwKBkWh? M1nCS2ROW09? MkLlTWM2OD15Lkm0O{DPxE1? NETMWIozOjh{OUC5OC=>
KM-H2 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\RO|LjiImq MoXYSG1UVw>? MnvOTWM2OD1zLkOwPEDPxE1? MXuyNlgzQTB7NB?=
L-540 NEj3fHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknrO|LjiImq MV\EUXNQ M3O5WmlEPTB;OD6yNVYh|ryP NFS3XZQzOjh{OUC5OC=>
HD-LM2 MnvWSpVv[3Srb36gRZN{[Xl? Ml7TNE4yNzBwNT:xM|Uh|ryP MYS3NwKBkWh? MW\EUXNQ NYTsUoRGcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? MXeyNlgzQTB7NB?=
L-428 MknrSpVv[3Srb36gRZN{[Xl? NEXHN3MxNjFxMD61M|EwPSEQvF2= M{L6OFcz6oDLaB?= M{i3XmROW09? MXTpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> M1\XfVIzQDJ7MEm0
KM-H2 MnjKSpVv[3Srb36gRZN{[Xl? MmPPNE4yNzBwNT:xM|Uh|ryP NFjoZpc4OuLCiXi= NXz4UZBYTE2VTx?= MW\pcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> NHfYeoIzOjh{OUC5OC=>
L-540 Mlz3SpVv[3Srb36gRZN{[Xl? M{PnNlAvOS9yLkWvNU82KM7:TR?= M4X6Z|cz6oDLaB?= NX21bmVtTE2VTx?= MVLpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=> NGrSSJMzOjh{OUC5OC=>
HD-LM2 Mon4RZBweHSxc3nzJGF{e2G7 NHrKSWYyNzVizszN MoHjO|LjiImq M2SxRmROW09? MmLSbY5lfWOnczDhdI9xfG:|aYO= MVWyNlgzQTB7NB?=
L-428 NIe3c4VCeG:ydH;zbZMhSXO|YYm= MYGxM|Uh|ryP MUS3NwKBkWh? MYnEUXNQ NV3zRZp2cW6mdXPld{BieG:ydH;zbZM> NHvydYkzOjh{OUC5OC=>
KM-H2 NXr4[WRWSXCxcITvd4l{KEG|c3H5 M1fhSVEwPSEQvF2= NFG1SpI4OuLCiXi= M4niWmROW09? NFH6b|VqdmS3Y3XzJIFxd3C2b4Ppdy=> NX7iN4w{OjJ6MkmwPVQ>
L-540 NF7WUWpCeG:ydH;zbZMhSXO|YYm= M1HsU|EwPSEQvF2= NYK5d2FbPzMkgJno NHLsenZFVVOR NUHTXpBkcW6mdXPld{BieG:ydH;zbZM> NFfKbpYzOjh{OUC5OC=>
U251-MG NV\RXmhETnWwY4Tpc44hSXO|YYm= MVmxJOK2VQ>? MW[wMVE3KGh? NWn0O|Y5cW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w MorsNlIxOjd4OUG=
U87-MG NUHQeFBOTnWwY4Tpc44hSXO|YYm= M4TCb|EhyrWP Mof6NE0yPiCq NFLDUWdqdmirYnn0d{Bkd26|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25? MlyyNlIxOjd4OUG=
4C8 NUjwRWR4TnWwY4Tpc44hSXO|YYm= MXuxJOK2VQ>? NWDTbYxyOC1zNjDo MUnpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44> NUCzdZJtOjJyMke2PVE>
U251-MG MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV6xM|ExKML3TR?= NGj5NIYzPC92OD:3NkBp NUnaOWU6cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1? NWrZdXI4OjJyMke2PVE>
U87-MG M1Lp[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LCbFEwOTBiwsXN MoDjNlQwPDhxN{KgbC=> Mn7DbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIF1KGFiY3;uZ4VvfHKjdHnvckBw\iBzMDFCuW0> NFj6WZAzOjB{N{[5NS=>
4C8 MnXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLyOmVNOS9zMDFCuW0> M3fyV|I1NzR6L{eyJIg> MXLpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZZQh[SClb37j[Y51emG2aX;uJI9nKDFyINM1US=> NIjiRogzOjB{N{[5NS=>
U266 NYO2bWU3SXCxcITvd4l{KEG|c3H5 MWKwMlUuOiEQvF2= Mo[zOFgwPzJiaB?= M{XBeolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NGexdXQzOTF4NEWxOy=>
Kms.11 Mn[5RZBweHSxc3nzJGF{e2G7 NVvhUHdwOC53LUKg{txO NWriS2hQPDhxN{KgbC=> NH63NJVqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 Mk\vNlEyPjR3MUe=
8226 MnHERZBweHSxc3nzJGF{e2G7 NWPmZXgxOC53LUKg{txO NYLJRpRWPDhxN{KgbC=> MnLpbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MV2yNVE3PDVzNx?=

... Click to View More Cell Line Experimental Data

In vivo試験 AZD1480 inhibits the STAT3 phosphorylation in an xenograft model of human solid tumors and multiple myeloma. [1] In vivo, AZD1480 inhibits the growth of subcutaneous tumors and increases survival of mice bearing intracranial glioblastoma (GBM) tumors by inhibiting STAT-3 activity, indicating that pharmacologic inhibition of the JAK/STAT-3 pathway by AZD1480 should be considered for study in the treatment of patients with GBM tumors. [3]AZD1480 blocks lung infiltration of myeloid cells and formation of pulmonary metastases in both mouse syngeneic experimental and spontaneous metastatic models. Furthermore, AZD1480 reduces angiogenesis and metastasis in a human xenograft tumor model. [4] The Jak2 inhibitor, AZD1480, suppresses the growth of human solid tumor xenografts harboring persistent Stat3 activity. [5]
臨床試験 AZD1480 is currently in Phase I clinical trials in Asian Patients With Advanced Solid Malignancies and Asian Patients With Advanced Hepatocellular Carcinoma (HCC)
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [5]

kinase assays Inhibition studies of AZD1480 are performed using recombinant Jak1, Jak2, or Jak3 under buffer conditions of 50 mM HEPES pH 7.3, 1 mM DTT, 0.01% Tween-20, 50 mM/ml BSA, and 10 mM MgCl2. Jak3 enzyme is expressed as N-terminal GST fusion in insect cells and purified by glutathione-affinity and size-exclusion chromatographies. Enzymes are assayed in the presence of AZD1480 (10 point dose response, in triplicate, from 8.3 μM to 0.3 nM in half-log dilution steps) using 1.5 μM peptide substrate (Jak1: FITC-C6-KKHTDDGYMPMSPGVA-NH2, Jak2 and Jak3: FAM-SRCtide) and screened under their respective ATP Km (Jak1: 55 μM, Jak2: 15 μM, Jak3: 3 μM) and approximated physiological ATP concentration of 5 mM. Phosphorylated and unphosphorylated peptides are separated and quantified by a Caliper LC3000 system for calculating percent inhibition.

細胞アッセイ: [4]

細胞株 Renca or 786-O cells, mouse endothelial cells and splenic CD11b+/c-myeloid cells, HUVECs
濃度 ~1 μM
反応時間 48 or 24 hours
実験の流れ Renca or 786-O cells are suspended in DMEM medium with 5% FBS , and seeded in 96-well plates (5×103 per well) to allow adhesion and then treated with DMSO or AZD1480 for 48 hours. Cell viability is determined by MTS assay. Absorbance at 490 nm is measured with Mikrotek Laborsysteme. Mouse endothelial cells and splenic CD11b+/c- myeloid cells are enriched from tumor-bearing mice,and cultured in 5% FBS RPMI-1640 medium. HUVECs are cultured on collagen 1–coated plates in complete medium. All cells are treated with DMSO and AZD1480 at various doses for 24 hours. Cell viability is determined by counting cell number manually. All the experiments are repeated 3 times.

動物実験: [4]

動物モデル Female BALB/c and athymic nude (NCR - nu/nu) mice (7–8 weeks old)
製剤 AZD1480 is suspended in water supplemented with 0.5% hypromellose and 0.1% Tween 80.
投薬量 Once a day at the dose of 50 mg/kg or twice daily at 30 mg/kg
投与方法 Oral gavage

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download AZD1480 SDF
分子量 348.77
化学式

C14H14ClFN8

CAS No. 935666-88-9
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 69 mg/mL warmed (197.83 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 5 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 (S)-5-chloro-N2-(1-(5-fluoropyrimidin-2-yl)ethyl)-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine

カスタマーフィードバック (2)


Click to enlarge
Rating
Source , , Nat Cell Biol, 2015, 17(1): 57-67. AZD1480 purchased from Selleck
Method bDNA Analysis
Cell Lines PSC-WA
Concentrations 0.1-5 μM
Incubation Time
Results Three other JAK1/2 inhibitors, AZD1480, CYT387 and Baricitinib, also showed up-regulation of UCP1 expression.

Click to enlarge
Rating
Source M.Sc. Karoline Gaebler and Dr. Claude Haan of Université du Luxembour. AZD1480 purchased from Selleck
Method Western blot
Cell Lines HEL cells
Concentrations 0-10 μM
Incubation Time 3 h
Results AZD1480 inhibits Jak2-V617F mediated signal transduction at micromolar concentrations in intact cells.

文献中の引用 (12)

技術サポート&よくある質問(FAQ)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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