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

Properties

• Quality Level: 100
• 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

Description

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.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable