A pan-Pim kinase inhibitor
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AZD 1208

Item No. 20235

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(5Z)-[[2-[(3R)-3-amino-1-piperidinyl][1,1'-biphenyl]-3-yl]methylene]-2,4-thiazolidinedione
CAS Number
1204144-28-4
Molecular Formula
C21H21N3O2S
Formula Weight
379.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.1 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml
λmax
230, 327 nm
SMILES
O=C(N1)S/C(C1=O)=C\C2=C(N3CCC[C@@H](N)C3)C(C4=CC=CC=C4)=CC=C2
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    AZD 1208 is a potent, selective, and orally available inhibitor of all three forms of the proto-oncogene Pim kinase (IC50s = 0.4, 5.0, and 1.9 nM for Pim-1, Pim-2, and Pim-3, respectively).1 It causes cell cycle arrest and apoptosis in MOLM-16 megakaryoblastic leukemia cells and inhibits the growth of MOLM-16 xenograft tumors in mice.1 It has efficacy against acute myeloid leukemia and glioblastoma cells when combined with mTOR and p110α inhibitors, respectively.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Keeton, E.K., McEachern, K., Dillman, K.S., et al. AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia. Blood 123(6), 905-913 (2014).

    2. Harada, M., Benito, J., Yamamaoto, S., et al. The novel combination of dual mTOR inhibitor AZD2014 and pan-PIM inhibitor AZD1208 inhibits growth in acute myeloid leukemia via HSF pathway suppression. Oncotarget 6(35), 37930-37947 (2015).

    3. Iqbal, A., Eckerdt, F., Bell, J., et al. Targeting of glioblastoma cell lines and glioma stem cells by combined PIM kinase and PI3K-p110α inhibition. Oncotarget 7(22), 33192-33201 (2016).