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:
Molecular Weight:
354.36
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality Segment
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
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
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
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