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Merck
CN

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:
1204144-28-4
Molecular Weight:
379.48
MDL number:
MFCD25976757
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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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

Related Categories

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 Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000463172
0000463172
0000423848
0000423848
0000417649

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Mehdi Bouhaddou et al.
Cell, 182(3), 685-712 (2020-07-10)
The causative agent of the coronavirus disease 2019 (COVID-19) pandemic, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has infected millions and killed hundreds of thousands of people worldwide, highlighting an urgent need to develop antiviral therapies. Here we present a

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