AZD1480

Catalog No.S2162

Molecular Weight(MW): 348.77

AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1.

Cited by 30 Publications

Cell Stem Cell, 2019, 25(1):69-86

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Cell, 2018, 175(2):458-471

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Cancer Cell, 2018, 34(2):315-330

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Cancers (Basel), 2019, 11(1)

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Am J Physiol Lung Cell Mol Physiol, 2019, 316(3):L487-L497

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Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0254-4

PubMed: 31201357 ( click the link to review the publication )

Nat Commun, 2018, 9(1):4345

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Cancer Lett, 2018, 429:54-65

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Int J Obes , 2018, 42(2):252-259

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J Cell Sci, 2018, 131(10)

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Blood, 2017, 129(14):1969-1979

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Oxid Med Cell Longev, 2017, 2017:7601592

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Endocrinology, 2017, 158(7):2255-2268

PubMed: 28444169 ( click the link to review the publication )

Neuro Oncol, 2016, 10.1093/neuonc/now139

PubMed: 27402815 ( click the link to review the publication )

Biochim Biophys Acta, 2016, 1863(11):2758-2765

PubMed: 27566291 ( click the link to review the publication )

Photodiagnosis Photodyn Ther, 2016, 14:119-27

PubMed: 26607555 ( click the link to review the publication )

Nat Cell Biol, 2015, 17(1):57-67

PubMed: 25487280 ( click the link to review the publication )

Cell Rep, 2015, 10.1016/j.celrep.2015.04.049

PubMed: 26027934 ( click the link to review the publication )

Mol Pharmacol, 2015, 87(4):572-81

PubMed: ( click the link to review the publication )

Biochem Biophys Res Commun, 2015, 458(4):908-12

PubMed: 25704089 ( click the link to review the publication )

Biochem Biophys Res Commun, 2015, 458(4):908-12

PubMed: ( click the link to review the publication )

Blood, 2014, 123(10):1516-24

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Oncol Rep, 2014, 32(5):1991-8

PubMed: 25216185 ( click the link to review the publication )

PLoS One, 2014, 9(10):e109799

PubMed: 25289677 ( click the link to review the publication )
PLoS One, 2014, 9(11):e112014

PubMed: 25390891 ( click the link to review the publication )

Cancer Lett, 2013, 341(2):224-30

PubMed: 23941832 ( click the link to review the publication )

Endocrinology, 2013, 154(9):3219-27

PubMed: 23782942 ( click the link to review the publication )

Asian Pac J Cancer Prev, 2013, 14(8):4823-7

PubMed: 24083752 ( click the link to review the publication )

Leukemia, 2012, 26(4):708-15

PubMed: 21926964 ( click the link to review the publication )

Mol Cell Proteomics, 2012, 11(6):M112.017764

PubMed: 22345495 ( click the link to review the publication )

Purity & Quality Control

Choose Selective JAK Inhibitors

Biological Activity

Description

AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1.

Targets

JAK2 ^[1]
(Cell-free assay)

0.26 nM

In vitro

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 Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
SW620	MVzGeY5kfGmxbjDBd5NigQ>?	MX:1JO69VQ>?	M2\nVVQ5KGh?	M4DHfGROW09?	M2qzdoJtd2OtczDKRWszN1OWQWSzJJNq\26jbHnu[y=>	NV3HUmQyOjV7NUS5O\|Q>
LoVo	NWPOSph7TnWwY4Tpc44hSXO\|YYm=	MVu1JO69VQ>?	M3nJbVQ5KGh?	MkPkSG1UVw>?	NVHwT5VK[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o	MlHNNlU6PTR7N{S=
HN5	M{ntTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M4XWbFczKGh?		MYfFR\|UxRTNwOEGgxtEhOS57OTFOwG0>	M3KyOFI2QDFyMEGw
Cal33	MmjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NVrjUVdrPzJiaB?=		NHXTfpNGSzVyPUOuN\|chyrFiMD63OUDPxE1?	M3TtTVI2QDFyMEGw
UM-22B	M3vkN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NVr2U3V7PzJiaB?=		NGXEZ4dGSzVyPUKuOlYhyrFiMD6yOEDPxE1?	NFXzeGEzPThzMECxNC=>
686LN	NHziXIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NXSwbow3PzJiaB?=		MnS0SWM2OD1{LkC1JOKyKDFwM{Og{txO	NYjF[W9EOjV6MUCwNVA>
UM SCC-1	NV\RW4RsT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M{fCWFczKGh?		MlvDSWM2OD1zLk[3JOKyKDBwNEKg{txO	M1rDPFI2QDFyMEGw
UM-22A	Mn7tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NIi5[IE4OiCq		MYHFR\|UxRTFwM{KgxtEhOC5\|OTFOwG0>	NU\yZoVzOjV6MUCwNVA>
OSC19	MkTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M3TuRVczKGh?		NUTMNoR4TUN3ME2xMlI3KMLzIECuNlAh\|ryP	NEPuXG8zPThzMECxNC=>
PCI-52	NVjaU\|RiT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NITPNHk4OiCq		NUXoWmVkTUN3ME2xMlAxKMLzIECuNFkh\|ryP	M4rDVlI2QDFyMEGw
PCI-15B	MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M1exV\|czKGh?		NIHiSnFGSzVyPUCuPVkhyrFiMT63OEDPxE1?	NV3o[45wOjV6MUCwNVA>
UMSCC-1	NFzGc2dHfW6ldHnvckBCe3OjeR?=	NUPp[XFUOC5yMEC1MVEvPiEQvF2=	NGDYXnUzPCCq		MnLTZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	NFjVV4QzPThzMECxNC=>
Cal33	M2W0SmZ2dmO2aX;uJGF{e2G7	MWOwMlAxODVvMz64JO69VQ>?	NVTT[4xZOjRiaB?=		NUHieYJZ[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR\|VInyO\|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	NULifFkyOjV6MUCwNVA>
HH5	MkXTSpVv[3Srb36gRZN{[Xl?	MViwMlAxODVvMz64JO69VQ>?	NX[2eXJ[OjRiaB?=		NUHOTHZJ[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR\|VInyO\|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	MYCyOVgyODBzMB?=
UM-22A	NWrEeVFiTnWwY4Tpc44hSXO\|YYm=	MXmwMlAxODVvMT62JO69VQ>?	MWKyOEBp		NWH0SY1l[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR\|VInyO\|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	Mke1NlU5OTByMUC=
A1847	NUPKUZp[TnWwY4Tpc44hSXO\|YYm=	MkPDNE4xPS1zMDFOwG0>	MmHSNlQhcA>?	M3Xa[WROW00EoB?=	MXXy[YR2[2W\|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?=	NYDTdHV5OjV4NE[wNVU>
OVCAR-5	Mn;ISpVv[3Srb36gRZN{[Xl?	Mo\ZNE4xPS1zMDFOwG0>	NXjZcI53OjRiaB?=	NEOyPHFFVVORwrC=	M3;tOpJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz	NEPhWJgzPTZ2NkCxOS=>
OVCAR-8	M2TiZ2Z2dmO2aX;uJGF{e2G7	NGm1OosxNjB3LUGwJO69VQ>?	MkXTNlQhcA>?	M3;OSGROW00EoB?=	MnzEdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO=	MYiyOVY1PjBzNR?=
MOVCAR-5447	MXTGeY5kfGmxbjDBd5NigQ>?	NIm4do0xNjB3LUGwJO69VQ>?	M1HpXFI1KGh?	MVnEUXNQyqB?	NIDtblRz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=>	NHLaVHozPTZ2NkCxOS=>
MOVCAR-5009	NHW3[41HfW6ldHnvckBCe3OjeR?=	NGXGO3cxNjB3LUGwJO69VQ>?	NGfwU2EzPCCq	MliySG1UV8Li	M1Xh[JJm\HWlZYOgdIhwe3Cqb4L5cIF1\WRiU2TBWFMhdGW4ZXzz	MWOyOVY1PjBzNR?=
A1847	NY\KcZFlS2WubDDWbYFjcWyrdImgRZN{[Xl?	M3rpfFAvODVvMUCg{txO	NFPyPWk4OiCq	M3u0fWROW09?	MmnadoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2=	MV2yOVY1PjBzNR?=
OVCAR-5	MXnD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	MmnUNE4xPS1zMDFOwG0>	MY[3NkBp	Mo\lSG1UVw>?	MlLzdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2=	NFj3ZlYzPTZ2NkCxOS=>
OVCAR-8	NUjDZpBwS2WubDDWbYFjcWyrdImgRZN{[Xl?	MUSwMlA2NTFyIN88US=>	NXTENnFGPzJiaB?=	NFHuXIlFVVOR	NVHuS3NUemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0>	M2rEWlI2PjR4MEG1
OVCAR-5	MkLvRZBweHSxc3nzJGF{e2G7	M1\3cVAvPS9zL{Wg{txO	NFnqNGI1QCCq	NVTMfmRlTE2VTx?=	NUf1O2RWcW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=>	NWXKbot7OjV4NE[wNVU>
OVCAR-8	NIfUdG1CeG:ydH;zbZMhSXO\|YYm=	MV2wMlUwOS93IN88US=>	M{e3W\|Q5KGh?	M4rDU2ROW09?	MUHpcoR2[2W\|IIPp[45q\mmlYX70JIFxd3C2b4Ppd{BifCCqaXfoJINwdmOncn70doF1cW:w	MV:yOVY1PjBzNR?=
AKRSL	NEf3SlBE\WyuIG\pZYJqdGm2eTDBd5NigQ>?		NIjFVJE4OiCq		NF\GWpJKSzVy78{eNVAh\|ryP	MnX2NlU2ODR4M{W=
PALJDL	MWDD[YxtKF[rYXLpcIl1gSCDc4PhfS=>		NIW3RWw4OiCq		NFzk[JdKSzVyPUKuOEDPxE1?	MUCyOVUxPDZ\|NR?=
MO4	MVTGeY5kfGmxbjDBd5NigQ>?	NVjjOIVLOC53L{GvOUDPxE1?	NHjxblA3KGh?		M4TMNIlvcGmkaYTzJHAuW1SDVEOg[ZhxemW\|c3nvcuKh	NYnhWZRIOjVzNEm1N\|U>
DU145	MkX5SpVv[3Srb36gRZN{[Xl?	MonjNE0zODBibl2=	M{\lc\|EhcMLi		NEDwflh{fXCycnXzd4V{KEmOLU[tZYN1cX[jdHXkJHN1[XR\|IHHu[EBGWktzL{Kgd4lodmGuaX7n	NF\UTlAzPDV5N{m0Ni=>
DU145	M{L2Z2Z2dmO2aX;uJGF{e2G7	MkD3PFAxKG6P	M1vRflczKGh?		NUjJS2tPe3WycILld5NmeyCLTD22MYlv\HWlZXSgcYloemG2b4L5	MVKyOFU4Pzl2Mh?=
CWR22Rv1	M{G3UmZ2dmO2aX;uJGF{e2G7	M1ja[VgxOCCwTR?=	NFuxV5E4OiCq		Mny4d5VxeHKnc4Pld{BKVC14LXnu[JVk\WRibXnndoF1d3K7	NWLQSnMzOjR3N{e5OFI>
N592	M1jQ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MmPSTWM2OD1yLki0JO69VQ>?	MmH1NlQyPTh5MEG=
H82	NHHJR4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NXfZcos3UUN3ME2xMlM4KM7:TR?=	M37nRVI1OTV6N{Cx
GLC4	NHPsT2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MYjJR\|UxRTFwN{mg{txO	NHSwT3QzPDF3OEewNS=>
H526	MlPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M{fvWWlEPTB;Mz6wPEDPxE1?	NEH4UmMzPDF3OEewNS=>
H1173	M3W2Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NULKbWpiUUN3ME2yMlM6KM7:TR?=	NI\ESo8zPDF3OEewNS=>
DMS114	NVrDT2ZHT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M3TnSGlEPTB;MD63N{DPxE1?	MojsNlQyPTh5MEG=
NCI-N592	NGXCUZRHfW6ldHnvckBCe3OjeR?=	Mlv5NE4{NzFxMzFOwG0>	NVezcpZvOjRiaB?=		NEjncGlqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R?	NELsUXUzPDF3OEewNS=>
GLC4	M1[zc2Z2dmO2aX;uJGF{e2G7	M4riUVAvOy9zL{Og{txO	MXuyOEBp		MojnbY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1	MYKyOFE2QDdyMR?=
NCI-H82	MoTKSpVv[3Srb36gRZN{[Xl?	NX;uSIx{OC5\|L{GvN{DPxE1?	NI\E[WYzPCCq		M1XnNIlv\HWlZYOgS\|IwVSClZXzsJIN6[2ynIHHydoV{fA>?	NVXTbnFMOjRzNUi3NFE>
NCI-N592	NFThSVdCeG:ydH;zbZMhSXO\|YYm=	NF23em0xNjNxMT:zJO69VQ>?	NEDrdXA1QCCq		NXrWNYNEcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?=	NHXRbFYzPDF3OEewNS=>
GLC4	M{DLNmFxd3C2b4Ppd{BCe3OjeR?=	MXewMlMwOS9\|IN88US=>	MX60PEBp		M1LDeolv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN?	M1HufFI1OTV6N{Cx
NCI-H82	NXjiTFBRSXCxcITvd4l{KEG\|c3H5	M121TlAvOy9zL{Og{txO	Ml7DOFghcA>?		MXjpcoNz\WG\|ZYOgeIhmKGyndnXsJI9nKGOuZXH2[YQuS2G\|cHHz[UA{	NHyzPVQzPDF3OEewNS=>
CWR22Rv1	MUPBdI9xfG:\|aYOgRZN{[Xl?				NWTaNHo1UUN3ME2wMlQ5OiEQvF2=	NFfXToozOzl2MkC5OS=>
CWR22Pc	MlHwRZBweHSxc3nzJGF{e2G7				NEL1W41KSzVyPUCuOFM5KM7:TR?=	MoTxNlM6PDJyOUW=
PC-3	M{eyeGFxd3C2b4Ppd{BCe3OjeR?=				NHL0VGdKSzVyPUGuO\|U2KM7:TR?=	Ml3SNlM6PDJyOUW=
DU145	Mln6RZBweHSxc3nzJGF{e2G7				MoHsTWM2OD1\|LkWxO{DPxE1?	NYCwUIVsOjN7NEKwPVU>
RC165N	M2PEV2Fxd3C2b4Ppd{BCe3OjeR?=				M4exZ2lEPTB;Mj6wPFMh\|ryP	MV6yN\|k1OjB7NR?=
ARPE19	NH:xRYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MlnxSG1UVw>?	NHXQSHRKSzVyPUK0MlM5KM7:TR?=	NX;xSWpXOjN3M{G5NlE>
HEK293	NEfL[FVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MnvESG1UVw>?	NHzpVYVKSzVyPUiuOlch\|ryP	NEjSVo4zOzV\|MUmyNS=>
KCNR	M3jacGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NWfyOWVKTE2VTx?=	MY\JR\|UxRTBwNE[g{txO	NYqzToEzOjN3M{G5NlE>
SY5Y	MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MYTEUXNQ	NGDPcZRKSzVyPUCuN\|Yh\|ryP	MXeyN\|U{OTl{MR?=
BE2	M1TURmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NE\re2dFVVOR	NH7ISYdKSzVyPUCuO\|Eh\|ryP	NEnMOHUzOzV\|MUmyNS=>
AS	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			M3PBe2ROW09?	NWq0cpV1UUN3ME2xMlU{KM7:TR?=	M3\mPVI{PTNzOUKx
NGP	MoWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NXX5bFlwTE2VTx?=	MojFTWM2OD1yLkW2JO69VQ>?	NF\tUGszOzV\|MUmyNS=>
IMR32	MkPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M{LnN2ROW09?	NVfOOGJ4UUN3ME2wMlY3KM7:TR?=	M3nxR\|I{PTNzOUKx
LAN5	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NXXNTVZXTE2VTx?=	NVLNTotFUUN3ME2xMlA1KM7:TR?=	MVSyN\|U{OTl{MR?=
RH18	NEXvOHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MkPPSG1UVw>?	M17WWmlEPTB;MT60NkDPxE1?	M3HuRVI{PTNzOUKx
RH30	NEDrO4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NXPObYJ5TE2VTx?=	NInuRVNKSzVyPUGuNlUh\|ryP	M2[2WlI{PTNzOUKx
RH17	NXTsbFJpT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			M1vue2ROW09?	MXjJR\|UxRTJwNUGg{txO	MnGyNlM2OzF7MkG=
RH28	MmDwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M3Lt[mROW09?	MV\JR\|UxRTRwMkig{txO	M3XFVVI{PTNzOUKx
RH36	MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NUeyOFlrTE2VTx?=	MWrJR\|UxRTVwM{eg{txO	MWmyN\|U{OTl{MR?=
RH41	Mm\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NXPJclRXTE2VTx?=	MUDJR\|UxRTBwNEig{txO	MUGyN\|U{OTl{MR?=
RD	NGHUXplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M13QPWROW09?	MoHqTWM2OD12LkOyJO69VQ>?	Mk\NNlM2OzF7MkG=
TC32	NVGye457T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NHrEPIxFVVOR	MkfxTWM2OD1\|Lki1JO69VQ>?	Mn7jNlM2OzF7MkG=
TC71	M33iSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MnrmSG1UVw>?	NXXSRXRlUUN3ME20MlM{KM7:TR?=	NHvhfHMzOzV\|MUmyNS=>
KCNR	MknzRZBweHSxc3nzJGF{e2G7	NYjiWnZSOC53L{GuNE8zNjVizszN	Mn\NNlQhcA>?	NGr0PYlFVVOR	NVO0[GZLcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=>	NXrVTXc2OjN3M{G5NlE>
SY5Y	MUDBdI9xfG:\|aYOgRZN{[Xl?	MknLNE42NzFwMD:yMlUh\|ryP	NETuVoEzPCCq	MWPEUXNQ	M3nsb4lv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB\|L{egZYN1cX[rdIm=	NF64UVQzOzV\|MUmyNS=>
Rh18	M{HtdGFxd3C2b4Ppd{BCe3OjeR?=	MojMNE42NzFwMD:yMlUh\|ryP	NFvr[YYzPCCq	M2fufWROW09?	M3XXdolv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB\|L{egZYN1cX[rdIm=	NWPkWXB5OjN3M{G5NlE>
TC32	NX\NVJM{SXCxcITvd4l{KEG\|c3H5	MnfDNE42NzFwMD:yMlUh\|ryP	Mnv1NlQhcA>?	M{j2dGROW09?	NFq4[VVqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5	MkXzNlM2OzF7MkG=
KCNR	NYPMR\|VDTnWwY4Tpc44hSXO\|YYm=	NH7oXHIxNjVxMT6wM\|IvPS93IN88US=>	Ml7vNlQhcA>?	MkX6SG1UVw>?	M1TLN4lvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u	Mn\ONlM2OzF7MkG=
SY5Y	MnzNSpVv[3Srb36gRZN{[Xl?	NIi4PW4xNjVxMT6wM\|IvPS93IN88US=>	MYiyOEBp	NEL0U49FVVOR	Ml\WbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W\|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR\|IHHjeIl3[XSrb36=	NFHHZ28zOzV\|MUmyNS=>
Rh18	NXnZNG5[TnWwY4Tpc44hSXO\|YYm=	NETvb2sxNjVxMT6wM\|IvPS93IN88US=>	NIjKbVUzPCCq	NIS3PZRFVVOR	NYXaZoNLcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44>	M170cFI{PTNzOUKx
TC32	M4nQNGZ2dmO2aX;uJGF{e2G7	NYDXfGNbOC53L{GuNE8zNjVxNTFOwG0>	NW\jWXo5OjRiaB?=	MYfEUXNQ	MkjvbY5pcWKrdIOgZo91cCCnbnTv[4Vvd3W\|IHPvcpN1cXS3dHn2[UBidmRiSVytOk1qdmS3Y3XkJHNVSVR\|IHHjeIl3[XSrb36=	MkXzNlM2OzF7MkG=
TPC-1	M2LlOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MWSxJOK2VQ>?	MYKwMVQh\A>?	MkD5SG1UVw>?	Ml3KbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNkBlKHS{ZXH0cYVvfA>?	NGD6NlgzOzB3NkS5PS=>
MZ-CRC1	M2LRSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mmm1NUDDvU1?	MoPLNE02KGR?	NUHuPIlvTE2VTx?=	M130PYlvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFEh\CC2cnXheI1mdnR?	MoL4NlMxPTZ2OUm=
TT	NEflTFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWrufnpxOSEEtV2=	M{XZNlAuPCCm	MV\EUXNQ	NI\PfZNqdmirYnn0d{Bk\WyuIHfyc5d1cCCjZoTldkAyKGRidILlZZRu\W62	MnO5NlMxPTZ2OUm=
TPC-1	NWnmNGpzTnWwY4Tpc44hSXO\|YYm=	NV3ndYhiOSEEtV2=	M{LVelczKGh?	NWfXZok2TE2VTx?=	M4P3U4lv\HWlZYOgS\|Eh[myxY3vh[4U>	M{[2TVI{ODV4NEm5
MZ-CRC1	NI\Zbo5HfW6ldHnvckBCe3OjeR?=	Ml7jNUDDvU1?	M17tUFczKGh?	NWX5U29MTE2VTx?=	MVfpcoR2[2W\|IFexJIJtd2OtYXfl	NWXSb5lwOjNyNU[0PVk>
TT	M1LjO2Z2dmO2aX;uJGF{e2G7	NUfCR5ZPOSEEtV2=	Ml;UO\|IhcA>?	MnPkSG1UVw>?	M1PCfIlv\HWlZYOgS\|Eh[myxY3vh[4U>	MnWzNlMxPTZ2OUm=
MZ-CRC1	MYHBdI9xfG:\|aYOgRZN{[Xl?	Ml3mNUDDvU1?	MWS0PEBp	NYDU[FJwTE2VTx?=	MnvabY5lfWOnczDhdI9xfG:\|aYO=	Mni5NlMxPTZ2OUm=
TT	NEWyeFhCeG:ydH;zbZMhSXO\|YYm=	MUKxJOK2VQ>?	Ml;2OFghcA>?	M1nTbGROW09?	NHnMfXZqdmS3Y3XzJIFxd3C2b4Ppdy=>	NX7Mfnh3OjNyNU[0PVk>
HD-LM2	MlPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NVWwZmJuPzMkgJno	Mn[4SG1UVw>?	M{\acmlEPTB;Nz64OFQh\|ryP	MX2yNlgzQTB7NB?=
L-428	M3mzfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M3;4OVcz6oDLaB?=	NUHoTlVsTE2VTx?=	NV7SUJFrUUN3ME23Mlk1PyEQvF2=	MkWyNlI5OjlyOUS=
KM-H2	NX;Yeog6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NYLQTllEPzMkgJno	MUHEUXNQ	MV7JR\|UxRTFwM{C4JO69VQ>?	M{W1PVIzQDJ7MEm0
L-540	NFzx[pNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NVz3cZZ6PzMkgJno	NWPmV2RXTE2VTx?=	NYD2XotRUUN3ME24MlIyPiEQvF2=	MU[yNlgzQTB7NB?=
HD-LM2	NEDQ[mRHfW6ldHnvckBCe3OjeR?=	NYKzTI03OC5zL{CuOU8yNzVizszN	NIDydpI4OuLCiXi=	NVHzSmRxTE2VTx?=	M2nUR4lvcGmkaYTzJHNVSVR\|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v	MlfuNlI5OjlyOUS=
L-428	NV\TT3VHTnWwY4Tpc44hSXO\|YYm=	MXOwMlEwOC53L{GvOUDPxE1?	MlHyO\|LjiImq	MVHEUXNQ	NUfSfZF1cW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25?	NGW3fmozOjh{OUC5OC=>
KM-H2	MlTqSpVv[3Srb36gRZN{[Xl?	MYCwMlEwOC53L{GvOUDPxE1?	M4TINlcz6oDLaB?=	MYjEUXNQ	NUjWfFdXcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25?	M{LaZlIzQDJ7MEm0
L-540	M{TwTmZ2dmO2aX;uJGF{e2G7	M4fRblAvOS9yLkWvNU82KM7:TR?=	NXPXXWJVPzMkgJno	MYPEUXNQ	MXXpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=>	NGXGb2kzOjh{OUC5OC=>
HD-LM2	NHPuWlNCeG:ydH;zbZMhSXO\|YYm=	NVjjVHY4OS93IN88US=>	NI\YeHc4OuLCiXi=	NILVXmFFVVOR	NVq3[lk5cW6mdXPld{BieG:ydH;zbZM>	MWqyNlgzQTB7NB?=
L-428	NXLiO2V3SXCxcITvd4l{KEG\|c3H5	M3jETFEwPSEQvF2=	M{PtZlcz6oDLaB?=	NX3T[XRQTE2VTx?=	Mmi4bY5lfWOnczDhdI9xfG:\|aYO=	MYeyNlgzQTB7NB?=
KM-H2	NIH3WG5CeG:ydH;zbZMhSXO\|YYm=	M3iwZlEwPSEQvF2=	MkD3O\|LjiImq	M1fPV2ROW09?	NUjXdWlQcW6mdXPld{BieG:ydH;zbZM>	MkLzNlI5OjlyOUS=
L-540	MoLGRZBweHSxc3nzJGF{e2G7	NFTC[3AyNzVizszN	MXu3NwKBkWh?	NXLiWHUxTE2VTx?=	M{nK[olv\HWlZYOgZZBweHSxc3nz	NEHYRZUzOjh{OUC5OC=>
U251-MG	NF\KemxHfW6ldHnvckBCe3OjeR?=	MXixJOK2VQ>?	Ml3nNE0yPiCq		MmX5bY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v	NITDOHYzOjB{N{[5NS=>
U87-MG	NVXjTJFHTnWwY4Tpc44hSXO\|YYm=	NXznV\|FtOSEEtV2=	MmS5NE0yPiCq		MmLObY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v	NUmzVHVUOjJyMke2PVE>
4C8	NGXZNW1HfW6ldHnvckBCe3OjeR?=	MXOxJOK2VQ>?	NELqOJYxNTF4IHi=		NFHxVnBqdmirYnn0d{Bkd26\|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25?	MnT2NlIxOjd4OUG=
U251-MG	NGLlVJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWP3NlFFOS9zMDFCuW0>	M2LmXFI1NzR6L{eyJIg>		M4fQd4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBifCCjIHPvcoNmdnS{YYTpc44hd2ZiMUCgxtVO	MXOyNlAzPzZ7MR?=
U87-MG	MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXPwV5pmOS9zMDFCuW0>	MWCyOE81QC95MjDo		NYT6WVNScW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1?	NXj1N3FjOjJyMke2PVE>
4C8	NIG1W3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NULqTpFtOS9zMDFCuW0>	M2\UTFI1NzR6L{eyJIg>		NH\qboxqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>?	NHTBbVAzOjB{N{[5NS=>
U266	NHHFfnhCeG:ydH;zbZMhSXO\|YYm=	NFLtNWMxNjVvMjFOwG0>	NFXNSm41QC95MjDo		MnHWbY5lfWOnczDhdI9xfG:\|aYOg[I9{\SCmZYDlcoRmdnSueR?=	M2TFc\|IyOTZ2NUG3
Kms.11	NHez[ldCeG:ydH;zbZMhSXO\|YYm=	MX2wMlUuOiEQvF2=	NWfTe3p4PDhxN{KgbC=>		NFvjd29qdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5	NXTPWnZVOjFzNkS1NVc>
8226	NHP1N\|NCeG:ydH;zbZMhSXO\|YYm=	NHHmW5cxNjVvMjFOwG0>	NWntNnhkPDhxN{KgbC=>		M3HwXIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm=	NHLrTG0zOTF4NEWxOy=>

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-STAT3 / STAT3 / p-JAK2 / JAK2 ; PubMed: 22027691 Mol Cancer Ther 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 Blood Cancer J 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 Blood Cancer J 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 Front Endocrinol (Lausanne) 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 Mol Cancer Ther 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 Blood IL-3-independent Ba/F3 cells were treated with increasing concentrations of the JAK inhibitor AZD1480 showing submicromolar inhibition of proliferation.	22027691 25855603

In vivo

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]

Protocol

Kinase Assay:^[5]	+ Expand 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.
Cell Research:^[4]	+ Expand Cell lines: Renca or 786-O cells, mouse endothelial cells and splenic CD11b⁺/c^-myeloid cells, HUVECs Concentrations: ~1 μM Incubation Time: 48 or 24 hours Method: 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. (Only for Reference)
Animal Research:^[4]	+ Expand Animal Models: Female BALB/c and athymic nude (NCR ^- nu/nu) mice (7–8 weeks old) Formulation: AZD1480 is suspended in water supplemented with 0.5% hypromellose and 0.1% Tween 80. Dosages: Once a day at the dose of 50 mg/kg or twice daily at 30 mg/kg Administration: Oral gavage (Only for Reference)

References

+ Expand

Solubility (25°C)

In vitro	DMSO	69 mg/mL warmed (197.83 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% PEG400+0.5% Tween80+5% propylene glycol For best results, use promptly after mixing.	5 mg/mL

* 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.

Chemical Information Download AZD1480 SDF

Molecular Weight	348.77
Formula	C₁₄H₁₄ClFN₈
CAS No.	935666-88-9
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A

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JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

Pan JAK Inhibitor

Ruxolitinib (INCB018424) : Pan JAK1/2 inhibitor, IC50=3.3 nM/2.8 nM.
FDA-approved JAK Inhibitor

Tofacitinib (CP-690550,Tasocitinib) : Approved by FDA for rheumatoid arthritis (RA).
Newest JAK Inhibitor

XL019 ^New : Potent and selective JAK2 inhibitor with IC50 of 2.2 nM, exhibiting >50-fold selectivity over JAK1, JAK3 and TYK2.
Classic JAK Inhibitor

AG-490 (Tyrphostin B42) : Potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM; also potent to Aurora A/B, Abl(T315I). Phase 1/2.

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Cerdulatinib (PRT-062070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.
Ruxolitinib (INCB018424)

Ruxolitinib (INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3.
Tofacitinib (CP-690550) Citrate

Tofacitinib citrate (CP-690550 citrate) is a novel inhibitor of JAK with IC50 of 1 nM, 20 nM and 112 nM against JAK3, JAK2, and JAK1, respectively.
Tofacitinib (CP-690550,Tasocitinib)

Tofacitinib (CP-690550,Tasocitinib) is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1.
Fedratinib (SAR302503, TG101348)

Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Phase 2.
Momelotinib (CYT387)

Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Phase 3.
WP1066

WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. Phase 1.

Features:Similar to its parent compound AG490, WP1066 inhibits the phosphorylation of JAK2, but unlike AG490, WP1066 also degraded JAK2 protein.
Baricitinib (LY3009104, INCB028050)

Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Phase 3.

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AZD1480

Cited by 30 Publications

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Chemical Information Download AZD1480 SDF

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JAK Inhibitors with Unique Features

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AZD1480

Cited by 30 Publications

Purity & Quality Control

Choose Selective JAK Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download AZD1480 SDF

Bio Calculators

Molarity Calculator

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

Dilution Calculator

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

The Serial Dilution Calculator Equation

Serial Dilutions

Computed Result

Molecular Weight Calculator

Total Molecular Weight: g/mol

Instructions to calculate molar mass (molecular weight) of a chemical compound:

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molarity Calculator

Tech Support

JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

Related JAK Products

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)