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 MVzGeY5kfGmxbjDBd5NigQ>? MXi1JO69VQ>? NUTrdWRxPDhiaB?= M{[4Z2ROW09? MXricI9kc3NiSlHLNk9UXEGWMzDzbYdv[Wyrbne= M4TkS|I2QTV2OUe0
LoVo  MYnGeY5kfGmxbjDBd5NigQ>? MWi1JO69VQ>? M37CelQ5KGh? MWnEUXNQ M3zYWYJtd2OtczDKRWszN1OWQWSzJJNq\26jbHnu[y=> NXvkdI5FOjV7NUS5O|Q>
HN5 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrBSm9RPzJiaB?= NWjOZVRLTUN3ME2zMlgyKMLzIEGuPVkh|ryP MYiyOVgyODBzMB?=
Cal33 MlTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVu3NkBp MVTFR|UxRTNwM{egxtEhOC55NTFOwG0> MkiyNlU5OTByMUC=
UM-22B MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjufXFjPzJiaB?= MkTFSWM2OD1{Lk[2JOKyKDBwMkSg{txO NHfzPXQzPThzMECxNC=>
686LN Mm\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDxO|IhcA>? MV;FR|UxRTJwMEWgxtEhOS5|MzFOwG0> MYKyOVgyODBzMB?=
UM SCC-1 Mn;OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HyV|czKGh? M1Tx[mVEPTB;MT62O{DDuSByLkSyJO69VQ>? M4rHS|I2QDFyMEGw
UM-22A NW\QS|k1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFizWGw4OiCq NGPGU5pGSzVyPUGuN|IhyrFiMD6zPUDPxE1? NWWxOoxoOjV6MUCwNVA>
OSC19 NWXBb4tsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1yzT|czKGh? NGXTeGhGSzVyPUGuNlYhyrFiMD6yNEDPxE1? MViyOVgyODBzMB?=
PCI-52 NFvkT2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfGRVJDPzJiaB?= MoHPSWM2OD1zLkCwJOKyKDBwMEmg{txO M{jNUVI2QDFyMEGw
PCI-15B MoXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUW3NkBp MUXFR|UxRTBwOUmgxtEhOS55NDFOwG0> M3nzfVI2QDFyMEGw
UMSCC-1 MVjGeY5kfGmxbjDBd5NigQ>? NYj2SGRtOC5yMEC1MVEvPiEQvF2= MkOwNlQhcA>? M{TMO4Fjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MkHMNlU5OTByMUC=
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A1847 NIWzUZpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2q5Z|AvODVvMUCg{txO NWXNbZBYPzJiaB?= NU[4eZhbTE2VTx?= NHP2SYdz\WS3Y3XzJINmdGxidnnhZoltcXS7IHH0JJRp\SClb37j[ZJvfHKjdHnvckBw\iB3IN88US=> MlfINlU3PDZyMUW=
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AKRSL NGrDeVRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NWT5Zpc6PzJiaB?= NV\PNJN5UUN3MP-8olExKM7:TR?= NXLMXZRZOjV3MES2N|U>
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H1173 NYfHSnNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3foNmlEPTB;Mj6zPUDPxE1? MnTiNlQyPTh5MEG=
DMS114 Mm[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoD5TWM2OD1yLkezJO69VQ>? NXm2fGRuOjRzNUi3NFE>
NCI-N592 MkPnSpVv[3Srb36gRZN{[Xl? NE[1SVYxNjNxMT:zJO69VQ>? MWCyOEBp M2HEOIlv\HWlZYOgS|IwVSClZXzsJIN6[2ynIHHydoV{fA>? M37iUFI1OTV6N{Cx
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NCI-H82 MWTGeY5kfGmxbjDBd5NigQ>? MmfSNE4{NzFxMzFOwG0> NVe0NJNxOjRiaB?= MWfpcoR2[2W|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q> NWX2WHZnOjRzNUi3NFE>
NCI-N592 MYDBdI9xfG:|aYOgRZN{[Xl? NIW0U5cxNjNxMT:zJO69VQ>? NF31NlI1QCCq MWPpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G|cHHz[UA{ MmPLNlQyPTh5MEG=
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NCI-H82 NWHtfVB6SXCxcITvd4l{KEG|c3H5 MX:wMlMwOS9|IN88US=> MWW0PEBp NXXNS2dkcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?= M4Xyc|I1OTV6N{Cx
CWR22Rv1  NH\xWmlCeG:ydH;zbZMhSXO|YYm= MXvJR|UxRTBwNEiyJO69VQ>? M1O4eVI{QTR{MEm1
CWR22Pc NEDhWYtCeG:ydH;zbZMhSXO|YYm= MYrJR|UxRTBwNEO4JO69VQ>? MUiyN|k1OjB7NR?=
PC-3 NWPCWVR3SXCxcITvd4l{KEG|c3H5 MUDJR|UxRTFwN{W1JO69VQ>? MV:yN|k1OjB7NR?=
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ARPE19 MkHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfEUXNQ MkHrTWM2OD1{ND6zPEDPxE1? MUGyN|U{OTl{MR?=
HEK293 MnztS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnr2SG1UVw>? MlHITWM2OD16Lk[3JO69VQ>? NF7RO5QzOzV|MUmyNS=>
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RH36 M1fnfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnq5SG1UVw>? M2jSRWlEPTB;NT6zO{DPxE1? NHSzWpUzOzV|MUmyNS=>
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RD Mk\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\EfllFVVOR MnTSTWM2OD12LkOyJO69VQ>? NIrKOWwzOzV|MUmyNS=>
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TPC-1 MoLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljyNUDDvU1? NEPHOHQxNTRiZB?= MXzEUXNQ MmLLbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNkBlKHS{ZXH0cYVvfA>? MmXFNlMxPTZ2OUm=
MZ-CRC1  NI\qPZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LN[FEhyrWP NYS1WoxqOC13IHS= NVvuNGdnTE2VTx?= MmPNbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNUBlKHS{ZXH0cYVvfA>? NETjUGYzOzB3NkS5PS=>
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TPC-1 MnnxSpVv[3Srb36gRZN{[Xl? NVr3RldoOSEEtV2= M2\qclczKGh? MYXEUXNQ MUnpcoR2[2W|IFexJIJtd2OtYXfl NHPzW3MzOzB3NkS5PS=>
MZ-CRC1  M{TZbGZ2dmO2aX;uJGF{e2G7 NGrERYYyKML3TR?= M{DQcVczKGh? M2nVXWROW09? NWLPcmZOcW6mdXPld{BIOSCkbH;jb4Fo\Q>? M3LCclI{ODV4NEm5
TT  M1XLWGZ2dmO2aX;uJGF{e2G7 M4\VSVEhyrWP MoHsO|IhcA>? MUXEUXNQ MkmzbY5lfWOnczDHNUBjdG:la3Hn[S=> M4DofFI{ODV4NEm5
MZ-CRC1  NV\4T5RuSXCxcITvd4l{KEG|c3H5 M3TZOVEhyrWP NEj1OG41QCCq M2q4OWROW09? Mlv4bY5lfWOnczDhdI9xfG:|aYO= NUXHdXdKOjNyNU[0PVk>
TT  MkPuRZBweHSxc3nzJGF{e2G7 MmnINUDDvU1? M37lPFQ5KGh? M1fSOWROW09? MXnpcoR2[2W|IHHwc5B1d3Orcx?= MWeyN|A2PjR7OR?=
HD-LM2 MoDmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYO3NwKBkWh? NHLhSZZFVVOR NFPxU2pKSzVyPUeuPFQ1KM7:TR?= NVvKVW1yOjJ6MkmwPVQ>
L-428 M3HENmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWK1bYJiPzMkgJno NFe3UnRFVVOR NHS0XJdKSzVyPUeuPVQ4KM7:TR?= Ml;tNlI5OjlyOUS=
KM-H2 NY\jfY1YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NES1Oo44OuLCiXi= MVrEUXNQ NVy5WFBQUUN3ME2xMlMxQCEQvF2= MViyNlgzQTB7NB?=
L-540 NUf3d2gxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnsO|LjiImq M1[1WWROW09? NV\uZlBHUUN3ME24MlIyPiEQvF2= NV6zOFgyOjJ6MkmwPVQ>
HD-LM2 M{PKfGZ2dmO2aX;uJGF{e2G7 MoTjNE4yNzBwNT:xM|Uh|ryP M{PtSFcz6oDLaB?= MYHEUXNQ M2P4d4lvcGmkaYTzJHNVSVR|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v NFnYSHIzOjh{OUC5OC=>
L-428 NWLmNI9qTnWwY4Tpc44hSXO|YYm= NF7E[JUxNjFxMD61M|EwPSEQvF2= MoDRO|LjiImq Mn3VSG1UVw>? MkXhbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44> MX[yNlgzQTB7NB?=
KM-H2 NHi1bY1HfW6ldHnvckBCe3OjeR?= NXPBRllGOC5zL{CuOU8yNzVizszN M1X1Wlcz6oDLaB?= NVrSPGNFTE2VTx?= NYWzZ49NcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25? NUfzc|BKOjJ6MkmwPVQ>
L-540 M{HRVGZ2dmO2aX;uJGF{e2G7 M1\mWlAvOS9yLkWvNU82KM7:TR?= NIHoc4c4OuLCiXi= M4TxfGROW09? NF3jVohqdmirYnn0d{BUXEGWMzygV3RCXDViYX7kJHNVSVR4IIDoc5NxcG:{eXzheIlwdg>? NV[0VJJ4OjJ6MkmwPVQ>
HD-LM2 NHzJZ2xCeG:ydH;zbZMhSXO|YYm= MmTuNU82KM7:TR?= NV:3SJI5PzMkgJno MWLEUXNQ NEjjV45qdmS3Y3XzJIFxd3C2b4Ppdy=> NUfBOW5xOjJ6MkmwPVQ>
L-428 MXfBdI9xfG:|aYOgRZN{[Xl? M4fJXFEwPSEQvF2= M2\4N|cz6oDLaB?= MVHEUXNQ NYPNe3lDcW6mdXPld{BieG:ydH;zbZM> MlG0NlI5OjlyOUS=
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... 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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