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Merck
CN

SML3784

AZ960

≥98% (HPLC)

Synonym(s):

(S)-5-Fluoro-2-(1-(4-fluorophenyl)ethylamino)-6-(5-methyl-1H-pyrazol-3-ylamino)nicotinonitrile, 5-Fluoro-2-[[(1S)-1-(4-fluorophenyl)ethyl]amino]-6-[(5-methyl-1H-pyrazol-3-yl)amino]-3-pyridinecarbonitrile, AZ 960, AZ-960

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About This Item

Empirical Formula (Hill Notation):
C18H16F2N6
CAS Number:
905586-69-8
Molecular Weight:
354.36
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD16621127

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SMILES string

Fc1c(nc(c(c1)C#N)N[C@@H](C)c3ccc(cc3)F)Nc2[nH]nc(c2)C

InChI

1S/C18H16F2N6/c1-10-7-16(26-25-10)23-18-15(20)8-13(9-21)17(24-18)22-11(2)12-3-5-14(19)6-4-12/h3-8,11H,1-2H3,(H3,22,23,24,25,26)/t11-/m0/s1

InChI key

SUNXHXDJOIXABJ-NSHDSACASA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Quality Level

100

Related Categories

Biochem/physiol Actions

ATP-competitive, potent and selective Janus-associated kinase 2 (JAK2) inhibitor.
AZ960 is an ATP-competitive, potent and selective Janus-associated kinase 2 inhibitor (JAK2 Ki = 0.45 nM with 15 μM ATP, 96% inhibition at 10 nM) with additional lower potency against TrkA/Aurora-A/ARK5 (91/73/65% inhibition at 10 nM; IC50 >100 nM against 72 other kinases). AZ960 exhibits JAK2-selective anti-proliferation potency (GI50 = 25, 214, 230, 279 nM using cells expression TEL-JAK2, -Tyk2, -JAK1, -JAK3, respectively) and inhibits cellular STAT5 phosphorylation in TEL-JAK2-expressing cells (IC50 = 15 nM) at a 15–30-fold potency than the TEL-JAK1, -JAK3, and -Tyk2 transfectants.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000265103
0000265102
0000247220
0000265102
0000265103

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High MMP-11 expression associated with low CD8+ T cells decreases the survival rate in patients with breast cancer
PLoS ONE, 16(5), e0252052-e0252052 (2021)
FAT10 stimulates the development of osteosarcoma by regulating the JAK/STAT signaling pathway
Journal of B.U.ON. : Official Journal of the Balkan Union of Oncology, 26(5), 2090-2096 (2021)
Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor
Bioorganic & Medicinal Chemistry, 24(19), 4647-4651 (2016)
Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2
The Journal of Biological Chemistry, 283(47), 32334-32343 (2008)
AZ960, a novel Jak2 inhibitor, induces growth arrest and apoptosis in adult T-cell leukemia cells
Molecular Cancer Therapeutics, 9(12), 3386-3395 (2010)
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