SML2595

AZD1208

≥98% (HPLC)

• Synonym(e): (5Z)-5-[[2-[(3R)-3-Amino-1-piperidinyl][1,1′-biphenyl]-3-yl]methylene]-2,4-thiazolidinedione, (R,Z)-5-((2-(3-Aminopiperidin-1-yl)biphenyl-3-yl)methylene)thiazolidine-2,4-dione, AZD 1208, AZD-1208
• Empirische Formel (Hill-System): C₂₁H₂₁N₃O₂S
• CAS-Nummer: 1204144-28-4
• Molekulargewicht: 379.48
• MDL-Nummer: MFCD25976757
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: −20°C
• SMILES String: S1\C(=C/c2c(c(ccc2)c4ccccc4)N3C[C@@H](CCC3)N)\C(=O)NC1=O
• InChI: 1S/C21H21N3O2S/c22-16-9-5-11-24(13-16)19-15(12-18-20(25)23-21(26)27-18)8-4-10-17(19)14-6-2-1-3-7-14/h1-4,6-8,10,12,16H,5,9,11,13,22H2,(H,23,25,26)/b18-12-/t16-/m1/s1
• InChIKey: MCUJKPPARUPFJM-UWCCDQBKSA-N

Beschreibung

Biochem./physiol. Wirkung

AZD1208 is an orally available, potent ATP-competitive pan-Pim kinase inhibitor (Pim-1/-2/-3 Ki = 0.1/1.92/0.4 nM; Pim-1/-2/-3 IC₅₀ = 0.4/5.0/1.9 nM with [ATP] = Km; Pim-1/-2/-3 IC₅₀ = 2.6/164/17 nM with [ATP] = 5 mM) wtih high target selectivity (by binding assay with a 442-kinase panel). AZD1208 exhibits selective antiproliferation potency against high Pim-1/-2-expressing AML cultures (GI50 in 72 h = 20 nM/MOLM-16, 60 nM/EOL-1, 300 nM/Kasumi-3, 600 nM/KG-1a, 900 nM/MV4-11) and displays in vivo efficacy against MOLM-16 xenograft tumor growth in mice (by 89% or 100%, respectively, with 10 or 30 mg/kg/day p.o.)

Orally available, potent, selective, ATP-competitive pan-Pim kinase inhibitor against Pim-dependent cancer proliferation in vitro and in vivo.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable