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 35 Publications

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

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

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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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Front Immunol, 2019, 1.1243055556

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

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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

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

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Nat Commun, 2019, 10(1):3601

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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

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Neuro Oncol, 2016, 10.1093/neuonc/now139

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

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Photodiagnosis Photodyn Ther, 2016, 14:119-27

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

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

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

PubMed: ( click the link to review the publication )
Biochem Biophys Res Commun, 2015, 458(4):908-12

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

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

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

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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

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

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

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

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

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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	NHfMWnhHfW6ldHnvckBCe3OjeR?=	Ml2xOUDPxE1?	Ml7iOFghcA>?	MUHEUXNQ	MWLicI9kc3NiSlHLNk9UXEGWMzDzbYdv[Wyrbne=	NUTXO5lrOjV7NUS5O\|Q>
LoVo	MlnsSpVv[3Srb36gRZN{[Xl?	NGmyVXc2KM7:TR?=	NHLBb4Y1QCCq	Mnz6SG1UVw>?	NFzvbXRjdG:la4OgTmFMOi:VVFHUN{B{cWewYXzpcoc>	NF34[YMzPTl3NEm3OC=>
HN5	M4q5W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		Mn25O\|IhcA>?		MXzFR\|UxRTNwOEGgxtEhOS57OTFOwG0>	MXKyOVgyODBzMB?=
Cal33	M{nwXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NHrMSpY4OiCq		NVXpXWZrTUN3ME2zMlM4KMLzIECuO\|Uh\|ryP	NXe3TGd7OjV6MUCwNVA>
UM-22B	NYDlRZg4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M3rIU\|czKGh?		Mn3qSWM2OD1{Lk[2JOKyKDBwMkSg{txO	NFTQPZIzPThzMECxNC=>
686LN	MmHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MoXzO\|IhcA>?		MmKzSWM2OD1{LkC1JOKyKDFwM{Og{txO	NFvYdFkzPThzMECxNC=>
UM SCC-1	NEC4[4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MXm3NkBp		NFrUdoJGSzVyPUGuOlchyrFiMD60NkDPxE1?	MnLiNlU5OTByMUC=
UM-22A	M2PUVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NGWyUIc4OiCq		NXHiNY1HTUN3ME2xMlMzKMLzIECuN\|kh\|ryP	MlnQNlU5OTByMUC=
OSC19	M3jJ[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M2XLVlczKGh?		MVjFR\|UxRTFwMk[gxtEhOC5{MDFOwG0>	M1uwWFI2QDFyMEGw
PCI-52	NFvndItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MofPO\|IhcA>?		NHrPZlFGSzVyPUGuNFAhyrFiMD6wPUDPxE1?	MXmyOVgyODBzMB?=
PCI-15B	NUTQXHBWT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MXS3NkBp		M3O1R2VEPTB;MD65PUDDuSBzLke0JO69VQ>?	NXvvPZAxOjV6MUCwNVA>
UMSCC-1	M3;zOmZ2dmO2aX;uJGF{e2G7	MlHoNE4xODB3LUGuOkDPxE1?	M1HRdVI1KGh?		MUXhZpJw\2G2ZYOgTWwuPuLCk3nu[JVk\WRidYCtdoVofWyjdHnvckBw\iCyU2TBWFNVgXJ5MEZCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy	NWXsdmZKOjV6MUCwNVA>
Cal33	M1XNdGZ2dmO2aX;uJGF{e2G7	M3TVWVAvODByNT2zMlgh\|ryP	NUnqOHdEOjRiaB?=		Ml;aZYJzd2ejdHXzJGlNNTckgKPpcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZicGPURXQ{XHm{N{C1xsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	MXqyOVgyODBzMB?=
HH5	NXPke2c{TnWwY4Tpc44hSXO\|YYm=	MXOwMlAxODVvMz64JO69VQ>?	MmXRNlQhcA>?		NVvHWoUy[WK{b3fheIV{KEmOLUdihLNqdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3[gdHNVSVR\|VInyO\|A2yqCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	NFPP[pAzPThzMECxNC=>
UM-22A	MmPlSpVv[3Srb36gRZN{[Xl?	MVuwMlAxODVvMT62JO69VQ>?	MlPzNlQhcA>?		NHfJb2Ri[nKxZ3H0[ZMhUUxvNvMAl4lv\HWlZXSgeZAuemWpdXzheIlwdiCxZjDwV3RCXDOWeYK3NFXDqGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	NFLQO28zPThzMECxNC=>
A1847	M{fTfWZ2dmO2aX;uJGF{e2G7	MX[wMlA2NTFyIN88US=>	NUny[ZNOOjRiaB?=	NULWN4pZTE2VT9Mg	MV7y[YR2[2W\|IIDoc5NxcG:{eXzheIVlKFOWQWSzJIxmfmWucx?=	NYfZVIVPOjV4NE[wNVU>
OVCAR-5	M4\ucGZ2dmO2aX;uJGF{e2G7	M1fUbFAvODVvMUCg{txO	NH\YVFYzPCCq	NY\iVWJ7TE2VT9Mg	NWXKeoFSemWmdXPld{BxcG:\|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM>	NVXK[G9WOjV4NE[wNVU>
OVCAR-8	NV2wbYh7TnWwY4Tpc44hSXO\|YYm=	NUXYNGNoOC5yNT2xNEDPxE1?	NGW1XG0zPCCq	Mo\tSG1UV8Li	MnrkdoVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO=	NIG4UJQzPTZ2NkCxOS=>
MOVCAR-5447	M2X5UGZ2dmO2aX;uJGF{e2G7	NG\TWFYxNjB3LUGwJO69VQ>?	NFGw[FUzPCCq	NWPycppITE2VT9Mg	NVTZV2JQemWmdXPld{BxcG:\|cHjvdplt[XSnZDDTWGFVOyCuZY\lcJM>	MmnXNlU3PDZyMUW=
MOVCAR-5009	MV7GeY5kfGmxbjDBd5NigQ>?	NXnTTlVIOC5yNT2xNEDPxE1?	M{nLcVI1KGh?	MmDTSG1UV8Li	Mmq3doVlfWOnczDwbI9{eGixconsZZRm\CCVVFHUN{Bt\X[nbIO=	MV6yOVY1PjBzNR?=
A1847	MnTvR4VtdCCYaXHibYxqfHliQYPzZZk>	NUTrVWh{OC5yNT2xNEDPxE1?	MmL3O\|IhcA>?	M4\lNGROW09?	NYTTTG9KemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0>	NHHncWczPTZ2NkCxOS=>
OVCAR-5	MW\D[YxtKF[rYXLpcIl1gSCDc4PhfS=>	NH;Gdo8xNjB3LUGwJO69VQ>?	MXi3NkBp	M13HTmROW09?	MoHMdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjdDD0bIUh[2:wY3XycpRz[XSrb36gc4YhPSEQvF2=	MmfuNlU3PDZyMUW=
OVCAR-8	MlSxR4VtdCCYaXHibYxqfHliQYPzZZk>	M2LmOVAvODVvMUCg{txO	MU[3NkBp	M1LBe2ROW09?	NUfnSZRyemWmdXPld{Bk\WyuII\pZYJqdGm2eTDheEB1cGViY3;uZ4VzdnS{YYTpc44hd2ZiNTFOwG0>	M1nZWVI2PjR4MEG1
OVCAR-5	MlrDRZBweHSxc3nzJGF{e2G7	Ml25NE42NzFxNTFOwG0>	MnLDOFghcA>?	NGq3N4xFVVOR	MoPKbY5lfWOnczDzbYdvcW[rY3HueEBieG:ydH;zbZMh[XRiaHnnbEBkd26lZYLueJJifGmxbh?=	MYKyOVY1PjBzNR?=
OVCAR-8	M2jGfWFxd3C2b4Ppd{BCe3OjeR?=	MUCwMlUwOS93IN88US=>	NFvOVlg1QCCq	NYjBfW9ZTE2VTx?=	NXPWd\|F1cW6mdXPld{B{cWewaX\pZ4FvfCCjcH;weI9{cXNiYYSgbIlocCClb37j[ZJvfHKjdHnvci=>	M2OwbVI2PjR4MEG1
AKRSL	NH7PS3hE\WyuIG\pZYJqdGm2eTDBd5NigQ>?		NUnhVnlJPzJiaB?=		NYTJW5hWUUN3MP-8olExKM7:TR?=	NGOxcVkzPTVyNE[zOS=>
PALJDL	NEDEOnBE\WyuIG\pZYJqdGm2eTDBd5NigQ>?		MX63NkBp		NXLoSow6UUN3ME2yMlQh\|ryP	NF;BbYMzPTVyNE[zOS=>
MO4	MXzGeY5kfGmxbjDBd5NigQ>?	NXvQb3VtOC53L{GvOUDPxE1?	MUm2JIg>		MVTpcohq[mm2czDQMXNVSVR\|IHX4dJJme3Orb39CpC=>	NH2y[JEzPTF2OUWzOS=>
DU145	NWPncmFGTnWwY4Tpc44hSXO\|YYm=	Mn2yNE0zODBibl2=	MXexJIjDqA>?		MmHNd5VxeHKnc4Pld{BKVC14LXHjeIl3[XSnZDDTeIF1OyCjbnSgSXJMOS9{IIPp[45idGmwZx?=	NGXaRnozPDV5N{m0Ni=>
DU145	MkHISpVv[3Srb36gRZN{[Xl?	MmPwPFAxKG6P	NFzIV\|Q4OiCq		MYnzeZBxemW\|c3XzJGlNNTZvaX7keYNm\CCvaXfyZZRwenl?	NIXlc2MzPDV5N{m0Ni=>
CWR22Rv1	MYHGeY5kfGmxbjDBd5NigQ>?	NV;CeYJyQDByIH7N	NF3tRlQ4OiCq		NFHHcoV{fXCycnXzd4V{KEmOLU[tbY5lfWOnZDDtbYdz[XSxcom=	M{jRS\|I1PTd5OUSy
N592	MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				M2PoWGlEPTB;MD64OEDPxE1?	MXeyOFE2QDdyMR?=
H82	Ml;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MXXJR\|UxRTFwM{eg{txO	NFHvOpUzPDF3OEewNS=>
GLC4	NXTGW\|JwT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MnjQTWM2OD1zLke5JO69VQ>?	NIO4cFczPDF3OEewNS=>
H526	Mnm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NXPkb5JqUUN3ME2zMlA5KM7:TR?=	NImzS2EzPDF3OEewNS=>
H1173	NIXzdlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MYrJR\|UxRTJwM{mg{txO	NV;R[HBiOjRzNUi3NFE>
DMS114	M1Wwcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NEf1dnlKSzVyPUCuO\|Mh\|ryP	MmrlNlQyPTh5MEG=
NCI-N592	M{PlR2Z2dmO2aX;uJGF{e2G7	NYW0V3l6OC5\|L{GvN{DPxE1?	NFvVdHczPCCq		MVXpcoR2[2W\|IFeyM20h[2WubDDjfYNt\SCjcoLld5Q>	NVXEUFJnOjRzNUi3NFE>
GLC4	M1q3PGZ2dmO2aX;uJGF{e2G7	NGnCXmYxNjNxMT:zJO69VQ>?	M1fDTlI1KGh?		NEPnXWZqdmS3Y3XzJGczN01iY3XscEBkgWOuZTDhdpJme3R?	MVKyOFE2QDdyMR?=
NCI-H82	NGnB[otHfW6ldHnvckBCe3OjeR?=	NGfZVo8xNjNxMT:zJO69VQ>?	NYTFXIdNOjRiaB?=		NWXkZYpicW6mdXPld{BIOi:PIHPlcIwh[3mlbHWgZZJz\XO2	NIDDOlkzPDF3OEewNS=>
NCI-N592	MUDBdI9xfG:\|aYOgRZN{[Xl?	NUTJOpFuOC5\|L{GvN{DPxE1?	M13OT\|Q5KGh?		NYLXW2d[cW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDjcIVifmWmLVPhd5Bie2ViMx?=	MkTVNlQyPTh5MEG=
GLC4	NH\SUlBCeG:ydH;zbZMhSXO\|YYm=	NHri[5MxNjNxMT:zJO69VQ>?	NWjX[JVGPDhiaB?=		M1;Ibolv[3KnYYPld{B1cGVibHX2[Ywhd2ZiY3zlZZZm\C2FYYPwZZNmKDN?	NFXrOYgzPDF3OEewNS=>
NCI-H82	MXrBdI9xfG:\|aYOgRZN{[Xl?	MXOwMlMwOS9\|IN88US=>	MYS0PEBp		NIDRNZlqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIHPs[YF3\WRvQ3HzdIF{\SB\|	NXzubYZIOjRzNUi3NFE>
CWR22Rv1	MVjBdI9xfG:\|aYOgRZN{[Xl?				NWHETZlKUUN3ME2wMlQ5OiEQvF2=	NHrVOowzOzl2MkC5OS=>
CWR22Pc	MkmzRZBweHSxc3nzJGF{e2G7				NGDRXIlKSzVyPUCuOFM5KM7:TR?=	NFPwUHEzOzl2MkC5OS=>
PC-3	MXjBdI9xfG:\|aYOgRZN{[Xl?				M{jvb2lEPTB;MT63OVUh\|ryP	MmXUNlM6PDJyOUW=
DU145	MlnwRZBweHSxc3nzJGF{e2G7				M4O4TWlEPTB;Mz61NVch\|ryP	NUnGWXl4OjN7NEKwPVU>
RC165N	MoruRZBweHSxc3nzJGF{e2G7				MlLZTWM2OD1{LkC4N{DPxE1?	MmjQNlM6PDJyOUW=
ARPE19	NUTmS4Q4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			M2HzUWROW09?	M{XJcmlEPTB;MkSuN\|gh\|ryP	NVLIeGYyOjN3M{G5NlE>
HEK293	MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MUjEUXNQ	NVe3bYdwUUN3ME24MlY4KM7:TR?=	MVyyN\|U{OTl{MR?=
KCNR	NFzPOolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			Mom5SG1UVw>?	NYH0W4dmUUN3ME2wMlQ3KM7:TR?=	M2HLeVI{PTNzOUKx
SY5Y	MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MkLFSG1UVw>?	MYDJR\|UxRTBwM{[g{txO	MmPGNlM2OzF7MkG=
BE2	NXXzdGhCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			M{\B[mROW09?	NVnm[pJkUUN3ME2wMlcyKM7:TR?=	MYGyN\|U{OTl{MR?=
AS	NGTlO3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M3\MeGROW09?	M4fC[WlEPTB;MT61N{DPxE1?	NUfNOItEOjN3M{G5NlE>
NGP	NVf4fI9[T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NIC3c4JFVVOR	Ml\GTWM2OD1yLkW2JO69VQ>?	M1zXR\|I{PTNzOUKx
IMR32	NYXD[XF5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MlfSSG1UVw>?	MVXJR\|UxRTBwNk[g{txO	NXnMOIhTOjN3M{G5NlE>
LAN5	NYTpblh2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MWLEUXNQ	NWjaTJdtUUN3ME2xMlA1KM7:TR?=	NI\DbIMzOzV\|MUmyNS=>
RH18	MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MWTEUXNQ	MXTJR\|UxRTFwNEKg{txO	M2q3OVI{PTNzOUKx
RH30	NV;mcFh7T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			Mn24SG1UVw>?	MnPuTWM2OD1zLkK1JO69VQ>?	MlPjNlM2OzF7MkG=
RH17	NYPL[o5lT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NEjZW3VFVVOR	Mn;6TWM2OD1{LkWxJO69VQ>?	NEHOWmgzOzV\|MUmyNS=>
RH28	MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			Mn\PSG1UVw>?	MUnJR\|UxRTRwMkig{txO	NFjk[JEzOzV\|MUmyNS=>
RH36	NHi1fmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NUPoR4VKTE2VTx?=	NGnXbopKSzVyPUWuN\|ch\|ryP	M2rTfFI{PTNzOUKx
RH41	NULtV3RmT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MmfJSG1UVw>?	Mof4TWM2OD1yLkS4JO69VQ>?	NHHRcYMzOzV\|MUmyNS=>
RD	MlT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NHy3TpdFVVOR	MnvFTWM2OD12LkOyJO69VQ>?	MVqyN\|U{OTl{MR?=
TC32	MmjjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M3PwOWROW09?	M{PrRmlEPTB;Mz64OUDPxE1?	MV6yN\|U{OTl{MR?=
TC71	MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MmCxSG1UVw>?	MXvJR\|UxRTRwM{Og{txO	M3fqTFI{PTNzOUKx
KCNR	NYTWbHZRSXCxcITvd4l{KEG\|c3H5	NXzifGQ3OC53L{GuNE8zNjVizszN	MWSyOEBp	MoHrSG1UVw>?	NVXTWoRzcW6mdXPld{BidiCrbnPy[YF{\SCrbjDjZZNx[XOnIEOvO{Bi[3Srdnn0fS=>	MnfPNlM2OzF7MkG=
SY5Y	MX7BdI9xfG:\|aYOgRZN{[Xl?	NV;KUZBiOC53L{GuNE8zNjVizszN	NUP1[o1ROjRiaB?=	MY\EUXNQ	MX\pcoR2[2W\|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7	MYWyN\|U{OTl{MR?=
Rh18	NWjWdWZxSXCxcITvd4l{KEG\|c3H5	M1jYTlAvPS9zLkCvNk42KM7:TR?=	M3TwSFI1KGh?	M1jLUGROW09?	MYnpcoR2[2W\|IHHuJIlv[3KnYYPlJIlvKGOjc4Dhd4UhOy95IHHjeIl3cXS7	NYq0eWdKOjN3M{G5NlE>
TC32	NY\IOXdYSXCxcITvd4l{KEG\|c3H5	M{jUW\|AvPS9zLkCvNk42KM7:TR?=	NInyRWUzPCCq	NGrVS41FVVOR	M3\sVIlv\HWlZYOgZY4hcW6lcnXhd4UhcW5iY3HzdIF{\SB\|L{egZYN1cX[rdIm=	NFn1OGwzOzV\|MUmyNS=>
KCNR	MUfGeY5kfGmxbjDBd5NigQ>?	NV7ZPG1wOC53L{GuNE8zNjVxNTFOwG0>	NX3MbXZlOjRiaB?=	NIGzWYJFVVOR	NHvrWYtqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=>	MWOyN\|U{OTl{MR?=
SY5Y	NHnRbXlHfW6ldHnvckBCe3OjeR?=	MXOwMlUwOS5yL{KuOU82KM7:TR?=	MWWyOEBp	MnLXSG1UVw>?	NVHTXlNtcW6qaXLpeJMh[m:2aDDlcoRw\2Wwb4XzJINwdnO2aYT1eIl3\SCjbnSgTWwuPi2rbnT1Z4VlKFOWQWSzJIFkfGm4YYTpc44>	MUeyN\|U{OTl{MR?=
Rh18	M2fQZmZ2dmO2aX;uJGF{e2G7	MU[wMlUwOS5yL{KuOU82KM7:TR?=	MkCzNlQhcA>?	M4LPOWROW09?	MVXpcohq[mm2czDic5RpKGWwZH;n[Y5wfXNiY3;ud5RqfHW2aY\lJIFv\CCLTD22MYlv\HWlZXSgV3RCXDNiYXP0bZZifGmxbh?=	NV7wbGw1OjN3M{G5NlE>
TC32	NGTXT3hHfW6ldHnvckBCe3OjeR?=	Mk\5NE42NzFwMD:yMlUwPSEQvF2=	NFHlSIMzPCCq	NFrZUnlFVVOR	NIizXlNqdmirYnn0d{Bjd3SqIHXu[I9o\W6xdYOgZ49ve3SrdIX0bZZmKGGwZDDJUE03NWmwZIXj[YQhW1SDVEOgZYN1cX[jdHnvci=>	M3vGd\|I{PTNzOUKx
TPC-1	M1;Zfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYXle\|VMOSEEtV2=	MVWwMVQh\A>?	NHe2OldFVVOR	M1TQdolvcGmkaYTzJINmdGxiZ4Lve5RpKGGodHXyJFIh\CC2cnXheI1mdnR?	NXHkfW9UOjNyNU[0PVk>
MZ-CRC1	MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHyzTGsyKML3TR?=	MlrtNE02KGR?	NVrUZ5dtTE2VTx?=	Ml3wbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[W[2ZYKgNUBlKHS{ZXH0cYVvfA>?	NGjGbYkzOzB3NkS5PS=>
TT	MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NH3sXoMyKML3TR?=	NXHpcWhHOC12IHS=	NVy1XY5wTE2VTx?=	NV7pOpVscW6qaXLpeJMh[2WubDDndo94fGhiYX\0[ZIhOSCmIITy[YF1dWWwdB?=	MVyyN\|A2PjR7OR?=
TPC-1	MmK1SpVv[3Srb36gRZN{[Xl?	NWXBfoFCOSEEtV2=	NWHKd4xJPzJiaB?=	NYP6[2RGTE2VTx?=	NIfZOmlqdmS3Y3XzJGcyKGKub3PrZYdm	M2PCNVI{ODV4NEm5
MZ-CRC1	NYC3bWR5TnWwY4Tpc44hSXO\|YYm=	NEG3bo0yKML3TR?=	MVe3NkBp	NH2xOnlFVVOR	M2j6PIlv\HWlZYOgS\|Eh[myxY3vh[4U>	MlLLNlMxPTZ2OUm=
TT	NX\NVVZzTnWwY4Tpc44hSXO\|YYm=	M2HTfVEhyrWP	MXi3NkBp	M1X5cWROW09?	MXnpcoR2[2W\|IFexJIJtd2OtYXfl	NVT3VGVMOjNyNU[0PVk>
MZ-CRC1	M3z4ZmFxd3C2b4Ppd{BCe3OjeR?=	Ml7nNUDDvU1?	MkLCOFghcA>?	MVfEUXNQ	NHrkfIJqdmS3Y3XzJIFxd3C2b4Ppdy=>	NXXuR2V1OjNyNU[0PVk>
TT	NVH0emd5SXCxcITvd4l{KEG\|c3H5	M1nwbVEhyrWP	M3Twd\|Q5KGh?	MlznSG1UVw>?	Mmq3bY5lfWOnczDhdI9xfG:\|aYO=	NHfvdFMzOzB3NkS5PS=>
HD-LM2	NUHh[HNmT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M2ToZlcz6oDLaB?=	M13EdWROW09?	MlzwTWM2OD15Lki0OEDPxE1?	MXeyNlgzQTB7NB?=
L-428	MnHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NYLDSndYPzMkgJno	MYfEUXNQ	NEm3UZhKSzVyPUeuPVQ4KM7:TR?=	M4CwNVIzQDJ7MEm0
KM-H2	M1LQSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MnvzO\|LjiImq	MXLEUXNQ	MlfPTWM2OD1zLkOwPEDPxE1?	NU\q[VdGOjJ6MkmwPVQ>
L-540	NYnLRmNQT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		Mm\PO\|LjiImq	NWKwWml4TE2VTx?=	MmrhTWM2OD16LkKxOkDPxE1?	NXT1SXFoOjJ6MkmwPVQ>
HD-LM2	NUf3SHhxTnWwY4Tpc44hSXO\|YYm=	M4T6Z\|AvOS9yLkWvNU82KM7:TR?=	M2HnfVcz6oDLaB?=	MkSySG1UVw>?	MkjlbY5pcWKrdIOgV3RCXDNuIGPURXQ2KGGwZDDTWGFVPiCyaH;zdIhwenmuYYTpc44>	NHHuNXIzOjh{OUC5OC=>
L-428	M4jrTGZ2dmO2aX;uJGF{e2G7	NGm3W\|kxNjFxMD61M\|EwPSEQvF2=	M1TjVFcz6oDLaB?=	Ml\oSG1UVw>?	NXTpcIsycW6qaXLpeJMhW1SDVEOsJHNVSVR3IHHu[EBUXEGWNjDwbI9{eGixconsZZRqd25?	NGPCZVEzOjh{OUC5OC=>
KM-H2	Ml;1SpVv[3Srb36gRZN{[Xl?	MojXNE4yNzBwNT:xM\|Uh\|ryP	M{TE[lcz6oDLaB?=	MlfwSG1UVw>?	MUjpcohq[mm2czDTWGFVOyxiU2TBWFUh[W6mIGPURXQ3KHCqb4PwbI9zgWyjdHnvci=>	NUTVXotoOjJ6MkmwPVQ>
L-540	MV\GeY5kfGmxbjDBd5NigQ>?	MXiwMlEwOC53L{GvOUDPxE1?	M17z[Fcz6oDLaB?=	M1zlemROW09?	M1j1ZYlvcGmkaYTzJHNVSVR\|LDDTWGFVPSCjbnSgV3RCXDZicHjvd5Bpd3K7bHH0bY9v	MUWyNlgzQTB7NB?=
HD-LM2	M4XqOGFxd3C2b4Ppd{BCe3OjeR?=	M1iyWlEwPSEQvF2=	M{LYVlcz6oDLaB?=	M2PySGROW09?	NWP5Zm5WcW6mdXPld{BieG:ydH;zbZM>	NHzGW\|AzOjh{OUC5OC=>
L-428	MnL0RZBweHSxc3nzJGF{e2G7	NVToPIVXOS93IN88US=>	NUf3VnlNPzMkgJno	NIPzcW5FVVOR	MV;pcoR2[2W\|IHHwc5B1d3Orcx?=	MX6yNlgzQTB7NB?=
KM-H2	MYfBdI9xfG:\|aYOgRZN{[Xl?	MmDZNU82KM7:TR?=	NIfqTGY4OuLCiXi=	Ml62SG1UVw>?	MXHpcoR2[2W\|IHHwc5B1d3Orcx?=	Mkj0NlI5OjlyOUS=
L-540	Mlr4RZBweHSxc3nzJGF{e2G7	NGq4R5YyNzVizszN	MkXUO\|LjiImq	MlvjSG1UVw>?	M4PQUYlv\HWlZYOgZZBweHSxc3nz	NVfyNZJOOjJ6MkmwPVQ>
U251-MG	MlvXSpVv[3Srb36gRZN{[Xl?	M1fOUVEhyrWP	MWOwMVE3KGh?		MWnpcohq[mm2czDjc45{fGm2dYTpeoUhW1SDVD2zJIFv\CCMQVuyJIFkfGm4YYTpc44>	MoHzNlIxOjd4OUG=
U87-MG	MlPWSpVv[3Srb36gRZN{[Xl?	M{LUTlEhyrWP	NWLLUWVYOC1zNjDo		M2nHRolvcGmkaYTzJINwdnO2aYT1eIl3\SCVVFHUMVMh[W6mIFrBT\|Ih[WO2aY\heIlwdg>?	MX2yNlAzPzZ7MR?=
4C8	M{HZdmZ2dmO2aX;uJGF{e2G7	NHG2Z3oyKML3TR?=	NE\NdpQxNTF4IHi=		NHrkNnVqdmirYnn0d{Bkd26\|dHn0eZRqfmViU2TBWE0{KGGwZDDKRWszKGGldHn2ZZRqd25?	MV2yNlAzPzZ7MR?=
U251-MG	MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MV[xM\|ExKML3TR?=	NWnQ[Yo3OjRxNEivO\|IhcA>?		NHrv[\|VqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h[XRiYTDjc45k\W62cnH0bY9vKG:oIEGwJOK2VQ>?	NUn0Tmp4OjJyMke2PVE>
U87-MG	M{\CWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NF76TI8yNzFyINM1US=>	MXOyOE81QC95MjDo		MlTMbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIF1KGFiY3;uZ4VvfHKjdHnvckBw\iBzMDFCuW0>	M1rkU\|IzODJ5Nkmx
4C8	NHrxSolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYWxM\|ExKML3TR?=	NXvTcIw6OjRxNEivO\|IhcA>?		NVfWcZc6cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IHGgZ49v[2WwdILheIlwdiCxZjCxNEDDvU1?	MVGyNlAzPzZ7MR?=
U266	NVPtU\|g2SXCxcITvd4l{KEG\|c3H5	NFn4V3AxNjVvMjFOwG0>	Mn7HOFgwPzJiaB?=		MlnCbY5lfWOnczDhdI9xfG:\|aYOg[I9{\SCmZYDlcoRmdnSueR?=	MX2yNVE3PDVzNx?=
Kms.11	MVrBdI9xfG:\|aYOgRZN{[Xl?	MViwMlUuOiEQvF2=	M1nDZ\|Q5Nzd{IHi=		NIHx[W9qdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5	MYGyNVE3PDVzNx?=
8226	M3jSemFxd3C2b4Ppd{BCe3OjeR?=	MYqwMlUuOiEQvF2=	M2HpXFQ5Nzd{IHi=		M{jzWIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm=	NWn2NJpCOjFzNkS1NVc>

... 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

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JAK Signaling Pathway Map

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FDA-approved JAK Inhibitor

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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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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)

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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)

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AZD1480

Cited by 35 Publications

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Chemical Information Download AZD1480 SDF

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AZD1480

Cited by 35 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

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Molecular Weight Calculator

Total Molecular Weight: g/mol

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

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Molarity Calculator

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JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

Related JAK Products

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