AZD1480

Name: AZD1480
Brand: Selleck Chemicals
SKU: S2162
Rating: 5 (50 reviews)

For research use only. Not for use in humans.

Catalog No.S2162

50 publications

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.

Selleck's AZD1480 has been cited by 50 publications

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

PubMed: 31080136 ( click the link to review the publication )

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

PubMed: 30173917 ( click the link to review the publication )

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

PubMed: 30173917 ( click the link to review the publication )

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

PubMed: 30033091 ( click the link to review the publication )

Cell Metab, 2017, 25(6):1320-1333

PubMed: 28591635 ( click the link to review the publication )

Nat Med, 2015, 21(1):47-54

PubMed: 25485912 ( click the link to review the publication )

Nat Commun, 2019, 10(1):716

PubMed: 30755611 ( click the link to review the publication )

Nat Commun, 2019, 10(1):3601

PubMed: 31399589 ( click the link to review the publication )

Cancer Res, 2019, 10.1158/0008-5472.CAN-18-2808

PubMed: 31806641 ( click the link to review the publication )

Oncogene, 2019, 101038/s41388-019-1136-4

PubMed: 31804622 ( click the link to review the publication )

Cancers (Basel), 2019, 11(1)

PubMed: 30634502 ( click the link to review the publication )

Cancers (Basel), 2019, 11(9)

PubMed: 31540495 ( click the link to review the publication )

Front Immunol, 2019, 1.1243055556

PubMed: 31156620 ( click the link to review the publication )

Gastric Cancer, 2019, 22(3):486-496

PubMed: 30264329 ( click the link to review the publication )

Stem Cell Res Ther, 2019, 10(1):384

PubMed: 31842997 ( click the link to review the publication )

J Cell Mol Med, 2019, 23(6):4301-4312

PubMed: 30993883 ( click the link to review the publication )

Lab Invest, 2019, 99(12):1810-1821

PubMed: 31467427 ( click the link to review the publication )

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

PubMed: 30604628 ( click the link to review the publication )

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

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

FEBS Open Bio, 2019, 9(10):1689-1704

PubMed: 31314158 ( click the link to review the publication )

Nat Commun, 2018, 9(1):4345

PubMed: 30341316 ( click the link to review the publication )

Cancer Lett, 2018, 429:54-65

PubMed: 29729901 ( click the link to review the publication )

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

PubMed: 28925407 ( click the link to review the publication )

J Cell Sci, 2018, 131(10)

PubMed: 29678906 ( click the link to review the publication )
Blood, 2017, 129(14):1969-1979

PubMed: 28151428 ( click the link to review the publication )

Oxid Med Cell Longev, 2017, 2017:7601592

PubMed: 29147463 ( click the link to review the publication )

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

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

J Clin Invest, 2016, 126(4):1300-10

PubMed: 26927669 ( click the link to review the publication )

Nat Commun, 2016, 7:12428

PubMed: 27687249 ( click the link to review the publication )

Neuro Oncol, 2016, 10.1093/neuonc/now139

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

Hum Mol Genet, 2016, 25(1):9-23

PubMed: 26494904 ( 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: 25583084 ( 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 )

Oncotarget, 2015, 8(48):83457-83468

PubMed: 29137356 ( click the link to review the publication )

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

PubMed: 24408322 ( click the link to review the publication )

Autophagy, 2014, 10(7):1212-28

PubMed: 24813621 ( click the link to review the publication )

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	MnLDSpVv[3Srb36gRZN{[Xl?	M3frdVUh\|ryP	MnzlOFghcA>?	MWTEUXNQ	MlLIZoxw[2u\|IFrBT\|IwW1SDVEOgd4lodmGuaX7n	MorINlU6PTR7N{S=
LoVo	NFPUbWRHfW6ldHnvckBCe3OjeR?=	M1PyNVUh\|ryP	Ml7yOFghcA>?	MmLOSG1UVw>?	NYq5XpBs[myxY3vzJGpCUzJxU2TBWFMhe2mpbnHsbY5o	NULQUHQxOjV7NUS5O\|Q>
HN5	MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MkL4O\|IhcA>?		M2PCZ2VEPTB;Mz64NUDDuSBzLkm5JO69VQ>?	MXOyOVgyODBzMB?=
Cal33	NV;wc5RST3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NGjMSWQ4OiCq		NWrBOHdRTUN3ME2zMlM4KMLzIECuO\|Uh\|ryP	NUj6eIZ[OjV6MUCwNVA>
UM-22B	Ml;3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NXn4e41{PzJiaB?=		NIfuW2VGSzVyPUKuOlYhyrFiMD6yOEDPxE1?	MVuyOVgyODBzMB?=
686LN	MoizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NYOwfoN3PzJiaB?=		NYLT[Zh[TUN3ME2yMlA2KMLzIEGuN\|Mh\|ryP	MY[yOVgyODBzMB?=
UM SCC-1	NEnUUYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		Mly5O\|IhcA>?		Mn:0SWM2OD1zLk[3JOKyKDBwNEKg{txO	MViyOVgyODBzMB?=
UM-22A	MknzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NWDkS3ZvPzJiaB?=		NH22VWVGSzVyPUGuN\|IhyrFiMD6zPUDPxE1?	M3\pXlI2QDFyMEGw
OSC19	NEXXbphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NHnkO2I4OiCq		NXmwOlZrTUN3ME2xMlI3KMLzIECuNlAh\|ryP	M2XTRVI2QDFyMEGw
PCI-52	MoHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NIf3PXo4OiCq		MlHFSWM2OD1zLkCwJOKyKDBwMEmg{txO	MWeyOVgyODBzMB?=
PCI-15B	MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NYf6TVYyPzJiaB?=		MnnBSWM2OD1yLkm5JOKyKDFwN{Sg{txO	M1vlblI2QDFyMEGw
UMSCC-1	NHjldm9HfW6ldHnvckBCe3OjeR?=	M{DmT\|AvODByNT2xMlYh\|ryP	M{[5fFI1KGh?		M2rVT4Fjem:pYYTld{BKVC144pETbY5lfWOnZDD1dE1z\We3bHH0bY9vKG:oIIDTWGFVO1S7ckewOeKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	MkSyNlU5OTByMUC=
Cal33	NU[wWo5kTnWwY4Tpc44hSXO\|YYm=	M3TWblAvODByNT2zMlgh\|ryP	MmK2NlQhcA>?		NE\QUZNi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	NET0PJQzPThzMECxNC=>
HH5	NEHCOppHfW6ldHnvckBCe3OjeR?=	NYn2VIlMOC5yMEC1MVMvQCEQvF2=	M2jvTFI1KGh?		MoT0ZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	NFnYTZYzPThzMECxNC=>
UM-22A	NUT1WZdlTnWwY4Tpc44hSXO\|YYm=	NGXJcnYxNjByMEWtNU43KM7:TR?=	MlzaNlQhcA>?		NHrMWVdi[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	M4DPVVI2QDFyMEGw
A1847	NX;3U49{TnWwY4Tpc44hSXO\|YYm=	MoTVNE4xPS1zMDFOwG0>	NHrlR4EzPCCq	MlfGSG1UV8Li	MmLZdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO=	NYDmU\|FWOjV4NE[wNVU>
OVCAR-5	MlLGSpVv[3Srb36gRZN{[Xl?	M4KyVVAvODVvMUCg{txO	M3KwSFI1KGh?	M33hbWROW00EoB?=	NImzbopz\WS3Y3XzJJBpd3OyaH;yfYxifGWmIGPURXQ{KGyndnXsdy=>	MUWyOVY1PjBzNR?=
OVCAR-8	Mn3rSpVv[3Srb36gRZN{[Xl?	MluxNE4xPS1zMDFOwG0>	NH\ZVIozPCCq	MVHEUXNQyqB?	MWry[YR2[2W\|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?=	NFLk[nEzPTZ2NkCxOS=>
MOVCAR-5447	MXTGeY5kfGmxbjDBd5NigQ>?	M33neFAvODVvMUCg{txO	MVqyOEBp	NHLoOW5FVVORwrC=	MkfidoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO=	M3nkdFI2PjR4MEG1
MOVCAR-5009	M2LsTmZ2dmO2aX;uJGF{e2G7	NGHtbZkxNjB3LUGwJO69VQ>?	Mm\5NlQhcA>?	NWrE[YZnTE2VT9Mg	NVrId3poemWmdXPld{BxcG:\|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM>	M375OlI2PjR4MEG1
A1847	MkniR4VtdCCYaXHibYxqfHliQYPzZZk>	M3f0OlAvODVvMUCg{txO	NEfJNZc4OiCq	M{fWTmROW09?	MmG5doVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2=	M{e0TFI2PjR4MEG1
OVCAR-5	M2nCfWNmdGxiVnnhZoltcXS7IFHzd4F6	Ml\5NE4xPS1zMDFOwG0>	NWXGS2dxPzJiaB?=	M362bmROW09?	NXG1OVVuemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0>	NGTsR5IzPTZ2NkCxOS=>
OVCAR-8	M1TVSmNmdGxiVnnhZoltcXS7IFHzd4F6	MnW0NE4xPS1zMDFOwG0>	NVLyU3h1PzJiaB?=	M33pS2ROW09?	M4S3RZJm\HWlZYOgZ4VtdCC4aXHibYxqfHliYYSgeIhmKGOxbnPldo51emG2aX;uJI9nKDVizszN	M{GxTlI2PjR4MEG1
OVCAR-5	NVnhO3ZMSXCxcITvd4l{KEG\|c3H5	M3P6clAvPS9zL{Wg{txO	NYm5Z446PDhiaB?=	NHO4SHdFVVOR	MlvTbY5lfWOnczDzbYdvcW[rY3HueEBieG:ydH;zbZMh[XRiaHnnbEBkd26lZYLueJJifGmxbh?=	M3jLXFI2PjR4MEG1
OVCAR-8	MljmRZBweHSxc3nzJGF{e2G7	MUmwMlUwOS93IN88US=>	NHroSno1QCCq	NWDmUZgzTE2VTx?=	NFv4OVVqdmS3Y3XzJJNq\26rZnnjZY51KGGyb4D0c5NqeyCjdDDobYdpKGOxbnPldo51emG2aX;u	M3;6flI2PjR4MEG1
AKRSL	NIrCcXBE\WyuIG\pZYJqdGm2eTDBd5NigQ>?		MW[3NkBp		M4jtSWlEPTExvK6xNEDPxE1?	NIi3[HgzPTVyNE[zOS=>
PALJDL	MVnD[YxtKF[rYXLpcIl1gSCDc4PhfS=>		NILEVos4OiCq		NYD3XVNIUUN3ME2yMlQh\|ryP	NULqNZpsOjV3MES2N\|U>
MO4	NGTsT4dHfW6ldHnvckBCe3OjeR?=	MWSwMlUwOS93IN88US=>	NYLzOpBXPiCq		MUTpcohq[mm2czDQMXNVSVR\|IHX4dJJme3Orb39CpC=>	MUiyOVE1QTV\|NR?=
DU145	MmjYSpVv[3Srb36gRZN{[Xl?	MnXqNE0zODBibl2=	NYL6c2xmOSCqwrC=		NUmxUndCe3WycILld5NmeyCLTD22MYFkfGm4YYTl[EBUfGG2MzDhcoQhTVKNMT:yJJNq\26jbHnu[y=>	NGXVTmEzPDV5N{m0Ni=>
DU145	M2\zW2Z2dmO2aX;uJGF{e2G7	M2KyXVgxOCCwTR?=	MV:3NkBp		NFGwR3d{fXCycnXzd4V{KEmOLU[tbY5lfWOnZDDtbYdz[XSxcom=	MVqyOFU4Pzl2Mh?=
CWR22Rv1	NFv5eFJHfW6ldHnvckBCe3OjeR?=	MWC4NFAhdk1?	NH35dHA4OiCq		NUS2eJRZe3WycILld5NmeyCLTD22MYlv\HWlZXSgcYloemG2b4L5	MYqyOFU4Pzl2Mh?=
N592	NFv0UpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NYHGU2loUUN3ME2wMlg1KM7:TR?=	MYOyOFE2QDdyMR?=
H82	Mmj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NELUe4VKSzVyPUGuN\|ch\|ryP	NHjjSIczPDF3OEewNS=>
GLC4	M3rl[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				Moq3TWM2OD1zLke5JO69VQ>?	MnHHNlQyPTh5MEG=
H526	M{\h[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MVLJR\|UxRTNwMEig{txO	M3;pU\|I1OTV6N{Cx
H1173	Mn3oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MkXsTWM2OD1{LkO5JO69VQ>?	MUGyOFE2QDdyMR?=
DMS114	M4jWVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MVrJR\|UxRTBwN{Og{txO	NWTROmF4OjRzNUi3NFE>
NCI-N592	MVjGeY5kfGmxbjDBd5NigQ>?	MWSwMlMwOS9\|IN88US=>	NYnrelV{OjRiaB?=		MnftbY5lfWOnczDHNk9OKGOnbHygZ5lkdGViYYLy[ZN1	MWOyOFE2QDdyMR?=
GLC4	NVrmNIN3TnWwY4Tpc44hSXO\|YYm=	NX\wbYZ6OC5\|L{GvN{DPxE1?	MViyOEBp		MVzpcoR2[2W\|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q>	NY\rfpY1OjRzNUi3NFE>
NCI-H82	NUS1V3I{TnWwY4Tpc44hSXO\|YYm=	Mn3ENE4{NzFxMzFOwG0>	MnrnNlQhcA>?		M3Wzbolv\HWlZYOgS\|IwVSClZXzsJIN6[2ynIHHydoV{fA>?	Ml3pNlQyPTh5MEG=
NCI-N592	NUPzZppOSXCxcITvd4l{KEG\|c3H5	MYSwMlMwOS9\|IN88US=>	NVfQXWdxPDhiaB?=		M2nTUIlv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN?	NVfnZVZROjRzNUi3NFE>
GLC4	MVjBdI9xfG:\|aYOgRZN{[Xl?	NUfJTWtpOC5\|L{GvN{DPxE1?	NEToPI01QCCq		NWK4clR3cW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?=	M4\XeFI1OTV6N{Cx
NCI-H82	MnPDRZBweHSxc3nzJGF{e2G7	MYewMlMwOS9\|IN88US=>	MUe0PEBp		NXq1NWplcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?=	NInLfYwzPDF3OEewNS=>
CWR22Rv1	M1H5fWFxd3C2b4Ppd{BCe3OjeR?=				Ml3HTWM2OD1yLkS4NkDPxE1?	NXvkPHNsOjN7NEKwPVU>
CWR22Pc	MULBdI9xfG:\|aYOgRZN{[Xl?				NHLJTZJKSzVyPUCuOFM5KM7:TR?=	NHHiS4szOzl2MkC5OS=>
PC-3	M3rQRWFxd3C2b4Ppd{BCe3OjeR?=				MnvHTWM2OD1zLke1OUDPxE1?	NUjMUY5yOjN7NEKwPVU>
DU145	NHrPdXRCeG:ydH;zbZMhSXO\|YYm=				NF;3c41KSzVyPUOuOVE4KM7:TR?=	NVu0RoNSOjN7NEKwPVU>
RC165N	NID3S3NCeG:ydH;zbZMhSXO\|YYm=				NX2xdXNnUUN3ME2yMlA5OyEQvF2=	NYHWd5JyOjN7NEKwPVU>
ARPE19	NXLpZoc{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			M3nkU2ROW09?	MWjJR\|UxRTJ2LkO4JO69VQ>?	M4n0UlI{PTNzOUKx
HEK293	MmCxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MYPEUXNQ	MVXJR\|UxRThwNkeg{txO	M3fVblI{PTNzOUKx
KCNR	NYXZWZpET3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MonqSG1UVw>?	NWH2V\|RvUUN3ME2wMlQ3KM7:TR?=	NE\DemkzOzV\|MUmyNS=>
SY5Y	MnTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M4PX[GROW09?	M4LJOmlEPTB;MD6zOkDPxE1?	NFj2O\|QzOzV\|MUmyNS=>
BE2	MoK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MY\EUXNQ	NHzpRmFKSzVyPUCuO\|Eh\|ryP	M1zKTlI{PTNzOUKx
AS	NIG5SnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NE\wd2dFVVOR	M4HFXWlEPTB;MT61N{DPxE1?	M1jteFI{PTNzOUKx
NGP	NIruXIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NETNUWFFVVOR	MVHJR\|UxRTBwNU[g{txO	NYrnRYVuOjN3M{G5NlE>
IMR32	M3fveGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MmPWSG1UVw>?	NXzjeVhJUUN3ME2wMlY3KM7:TR?=	NIHwXZQzOzV\|MUmyNS=>
LAN5	MlTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MVvEUXNQ	Mk\mTWM2OD1zLkC0JO69VQ>?	NXHK[pRPOjN3M{G5NlE>
RH18	MmjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M4r6UWROW09?	MUfJR\|UxRTFwNEKg{txO	NVP3cW5YOjN3M{G5NlE>
RH30	Mn;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M4naXmROW09?	M4fSW2lEPTB;MT6yOUDPxE1?	MYeyN\|U{OTl{MR?=
RH17	MnvXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NVzjN4xJTE2VTx?=	NXrielc5UUN3ME2yMlUyKM7:TR?=	NYjafmM3OjN3M{G5NlE>
RH28	M1u5N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NWHnN3V[TE2VTx?=	Mnf5TWM2OD12LkK4JO69VQ>?	MV2yN\|U{OTl{MR?=
RH36	M3;WOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NIjHZVhFVVOR	M3;pd2lEPTB;NT6zO{DPxE1?	NGrGWpUzOzV\|MUmyNS=>
RH41	MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NITkOZhFVVOR	M1[wd2lEPTB;MD60PEDPxE1?	NU\CU29EOjN3M{G5NlE>
RD	MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NV\qXGdJTE2VTx?=	NIPnPXFKSzVyPUSuN\|Ih\|ryP	MV2yN\|U{OTl{MR?=
TC32	NF7KeYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NHz6W5ZFVVOR	M1LWVGlEPTB;Mz64OUDPxE1?	NF[5d2QzOzV\|MUmyNS=>
TC71	NXnLSYhGT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			M2PyXWROW09?	NUXJTIJTUUN3ME20MlM{KM7:TR?=	NVTQO2x7OjN3M{G5NlE>
KCNR	NVLkTppGSXCxcITvd4l{KEG\|c3H5	M1rSfVAvPS9zLkCvNk42KM7:TR?=	MnrhNlQhcA>?	MYHEUXNQ	NYW3dJpycW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=>	NVf6TWJjOjN3M{G5NlE>
SY5Y	M1HSZmFxd3C2b4Ppd{BCe3OjeR?=	NYH3O5Z1OC53L{GuNE8zNjVizszN	M37nc\|I1KGh?	NXvtVXhPTE2VTx?=	MXvpcoR2[2W\|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7	NFTFflIzOzV\|MUmyNS=>
Rh18	NIjGW4FCeG:ydH;zbZMhSXO\|YYm=	MX[wMlUwOS5yL{KuOUDPxE1?	MkPXNlQhcA>?	Mn7lSG1UVw>?	NUPJR4E1cW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=>	NXzM[IFqOjN3M{G5NlE>
TC32	M4\MbWFxd3C2b4Ppd{BCe3OjeR?=	NFL1VHoxNjVxMT6wM\|IvPSEQvF2=	MUmyOEBp	MVPEUXNQ	NGToNINqdmS3Y3XzJIFvKGmwY4LlZZNmKGmwIHPhd5Bie2ViMz:3JIFkfGm4aYT5	MkPJNlM2OzF7MkG=
KCNR	NGfzUIxHfW6ldHnvckBCe3OjeR?=	NV7BTlhROC53L{GuNE8zNjVxNTFOwG0>	MYWyOEBp	MoTWSG1UVw>?	MX\pcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?=	NYjWfopYOjN3M{G5NlE>
SY5Y	Mm\MSpVv[3Srb36gRZN{[Xl?	NWHTRpF4OC53L{GuNE8zNjVxNTFOwG0>	MkPINlQhcA>?	NGL3emxFVVOR	M1m5V4lvcGmkaYTzJIJwfGhiZX7kc4dmdm:3czDjc45{fGm2dYTpeoUh[W6mIFnMMVYucW6mdXPl[EBUXEGWMzDhZ5RqfmG2aX;u	NE\qTVYzOzV\|MUmyNS=>
Rh18	NXrnOolCTnWwY4Tpc44hSXO\|YYm=	NH3aZnAxNjVxMT6wM\|IvPS93IN88US=>	NGXlUWczPCCq	MnzjSG1UVw>?	MYXpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?=	NHu4T\|UzOzV\|MUmyNS=>
TC32	MUHGeY5kfGmxbjDBd5NigQ>?	M2OwNlAvPS9zLkCvNk42NzVizszN	MWGyOEBp	MXvEUXNQ	NXz0XpNjcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44>	NV3LT5pFOjN3M{G5NlE>
TPC-1	MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	Mo\WNUDDvU1?	M2HnWVAuPCCm	NE\ne2dFVVOR	M3H3VolvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFIh\CC2cnXheI1mdnR?	NUPMbG1kOjNyNU[0PVk>
MZ-CRC1	NUnmPWFYT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NET0NmwyKML3TR?=	MYCwMVUh\A>?	M1fOcWROW09?	M{fZO4lvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFEh\CC2cnXheI1mdnR?	NYrDUm43OjNyNU[0PVk>
TT	MkPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1vBeVEhyrWP	NICwRWMxNTRiZB?=	MWjEUXNQ	MknWbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNUBlKHS{ZXH0cYVvfA>?	Mnu2NlMxPTZ2OUm=
TPC-1	M3fZdWZ2dmO2aX;uJGF{e2G7	NHXlSpgyKML3TR?=	NXi0[Yl4PzJiaB?=	NX7zRnZjTE2VTx?=	NW\ZZWp6cW6mdXPld{BIOSCkbH;jb4Fo\Q>?	MoLwNlMxPTZ2OUm=
MZ-CRC1	MUTGeY5kfGmxbjDBd5NigQ>?	MXGxJOK2VQ>?	M4LRfVczKGh?	NWXTT5pyTE2VTx?=	NXvPW3NJcW6mdXPld{BIOSCkbH;jb4Fo\Q>?	MUCyN\|A2PjR7OR?=
TT	NEfFTFZHfW6ldHnvckBCe3OjeR?=	NIrsfIcyKML3TR?=	NVjDcnNVPzJiaB?=	MVzEUXNQ	NIjIVG9qdmS3Y3XzJGcyKGKub3PrZYdm	NXnRWYlsOjNyNU[0PVk>
MZ-CRC1	MkTHRZBweHSxc3nzJGF{e2G7	MnrnNUDDvU1?	M{HJNlQ5KGh?	M1\MNWROW09?	MX3pcoR2[2W\|IHHwc5B1d3Orcx?=	NIjr[pMzOzB3NkS5PS=>
TT	NHL0Z5dCeG:ydH;zbZMhSXO\|YYm=	MWCxJOK2VQ>?	NYnNRXo5PDhiaB?=	M2e3XWROW09?	MmPhbY5lfWOnczDhdI9xfG:\|aYO=	MmfQNlMxPTZ2OUm=
HD-LM2	MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M2HtcFcz6oDLaB?=	NF\ReFVFVVOR	NH\kS3dKSzVyPUeuPFQ1KM7:TR?=	NYf5PZdNOjJ6MkmwPVQ>
L-428	MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NYPCdVZPPzMkgJno	Ml33SG1UVw>?	NIfWXodKSzVyPUeuPVQ4KM7:TR?=	M1;rV\|IzQDJ7MEm0
KM-H2	M{XmTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NXXrT5J5PzMkgJno	M1vIWGROW09?	MVnJR\|UxRTFwM{C4JO69VQ>?	NWnwblh[OjJ6MkmwPVQ>
L-540	MlO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MkLlO\|LjiImq	NGq0RXRFVVOR	NEHD[\|FKSzVyPUiuNlE3KM7:TR?=	MX:yNlgzQTB7NB?=
HD-LM2	MXzGeY5kfGmxbjDBd5NigQ>?	Ml:2NE4yNzBwNT:xM\|Uh\|ryP	NW\RcIdKPzMkgJno	MUHEUXNQ	M3;5fIlvcGmkaYTzJHNVSVR\|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v	NIrjRoQzOjh{OUC5OC=>
L-428	NW\OfGVCTnWwY4Tpc44hSXO\|YYm=	MUGwMlEwOC53L{GvOUDPxE1?	MX63NwKBkWh?	NXnGeldITE2VTx?=	Ml;pbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44>	NWj5XJpSOjJ6MkmwPVQ>
KM-H2	NX3NVHp{TnWwY4Tpc44hSXO\|YYm=	MoDXNE4yNzBwNT:xM\|Uh\|ryP	MlXTO\|LjiImq	NVfofmhiTE2VTx?=	NWjJ[FhFcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25?	NGLmbmszOjh{OUC5OC=>
L-540	MoLnSpVv[3Srb36gRZN{[Xl?	MmjuNE4yNzBwNT:xM\|Uh\|ryP	MljLO\|LjiImq	NFfRTY5FVVOR	NWj5SlFWcW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25?	M1XWbFIzQDJ7MEm0
HD-LM2	M4f5PGFxd3C2b4Ppd{BCe3OjeR?=	M334b\|EwPSEQvF2=	M1q0fFcz6oDLaB?=	MoXaSG1UVw>?	NVPlbYtHcW6mdXPld{BieG:ydH;zbZM>	NX;pcFZzOjJ6MkmwPVQ>
L-428	M1XrbWFxd3C2b4Ppd{BCe3OjeR?=	NXLs[5hqOS93IN88US=>	NUT5SYlDPzMkgJno	M13WVmROW09?	M{\YO4lv\HWlZYOgZZBweHSxc3nz	NULIO2hJOjJ6MkmwPVQ>
KM-H2	Mn\QRZBweHSxc3nzJGF{e2G7	MXyxM\|Uh\|ryP	NVnaNZRKPzMkgJno	MkjDSG1UVw>?	NV3ITnVWcW6mdXPld{BieG:ydH;zbZM>	MkW0NlI5OjlyOUS=
L-540	MoW4RZBweHSxc3nzJGF{e2G7	NEPFSFAyNzVizszN	M{T0[\|cz6oDLaB?=	MVfEUXNQ	Mni0bY5lfWOnczDhdI9xfG:\|aYO=	M2XadFIzQDJ7MEm0
U251-MG	MWfGeY5kfGmxbjDBd5NigQ>?	MWixJOK2VQ>?	NUL5cGx5OC1zNjDo		MnXkbY5pcWKrdIOgZ49ve3SrdIX0bZZmKFOWQWStN{BidmRiSlHLNkBi[3SrdnH0bY9v	MmjENlIxOjd4OUG=
U87-MG	NGq3fYJHfW6ldHnvckBCe3OjeR?=	M1O3V\|EhyrWP	M{jUVlAuOTZiaB?=		NFXQZoNqdmirYnn0d{Bkd26\|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25?	M1PYOVIzODJ5Nkmx
4C8	MWrGeY5kfGmxbjDBd5NigQ>?	MoTsNUDDvU1?	MoXaNE0yPiCq		NYPrV2JicW6qaXLpeJMh[2:wc4TpeJV1cX[nIGPURXQuOyCjbnSgTmFMOiCjY4TpeoF1cW:w	NX3KcZRXOjJyMke2PVE>
U251-MG	NFuzV2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYSxM\|ExKML3TR?=	M4fHW\|I1NzR6L{eyJIg>		NEKzOnBqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>?	NVToXXoyOjJyMke2PVE>
U87-MG	Mn7qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MY[xM\|ExKML3TR?=	NHHueWIzPC92OD:3NkBp		MoHtbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIF1KGFiY3;uZ4VvfHKjdHnvckBw\iBzMDFCuW0>	MVKyNlAzPzZ7MR?=
4C8	M2nTd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MUGxM\|ExKML3TR?=	NEK2RoczPC92OD:3NkBp		MnPtbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIF1KGFiY3;uZ4VvfHKjdHnvckBw\iBzMDFCuW0>	MUCyNlAzPzZ7MR?=
U266	MnGyRZBweHSxc3nzJGF{e2G7	M1P6e\|AvPS1{IN88US=>	NVHOVGdDPDhxN{KgbC=>		MoTUbY5lfWOnczDhdI9xfG:\|aYOg[I9{\SCmZYDlcoRmdnSueR?=	NFzZSlkzOTF4NEWxOy=>
Kms.11	NF3WWGxCeG:ydH;zbZMhSXO\|YYm=	MXqwMlUuOiEQvF2=	MkjqOFgwPzJiaB?=		NFTJZXpqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5	NYTscnBZOjFzNkS1NVc>
8226	MVfBdI9xfG:\|aYOgRZN{[Xl?	NWCyeoZWOC53LUKg{txO	NVn5eoNLPDhxN{KgbC=>		MYPpcoR2[2W\|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7	NXnZVJVxOjFzNkS1NVc>

... 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]	- Collapse 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]	- Collapse 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]	- Collapse 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

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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
Smiles	CC(NC1=NC=C(Cl)C(=N1)NC2=N[NH]C(=C2)C)C3=NC=C(F)C=N3

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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.

Related JAK Products

FLLL32 ^New

FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM.
Cerdulatinib (PRT062070) ^New

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)

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 (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 (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