SML2595
AZD1208
≥98% (HPLC)
Synonym(s):
(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
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About This Item
Empirical Formula (Hill Notation):
C21H21N3O2S
CAS Number:
Molecular Weight:
379.48
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−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
InChI key
MCUJKPPARUPFJM-UWCCDQBKSA-N
Biochem/physiol Actions
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.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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