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Submit ReviewAZD 1208 is a potent pan Pim kinase inhibitor (IC50 values are 0.4, 1.9 and 5.0 nM for Pim-1, 3 and 2, respectively). Exhibits >43-fold higher affinity for Pim kinases over a range of other kinases. Induces cell cycle arrest and apoptosis in AML cell lines in vitro and inhibits growth of tumor xenografts in vivo. AZD 1208 downmodulates the expression of Mayaro virus (MAYV) structural protein E1 and non-structural protein 1 (nsP1), and it reduces MAYV replication in a dose-dependent manner in HeLa or HDFs cells. Chemosensitizer.
分子量 | 379.48 |
公式 | C21H21N3O2S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1204144-28-4 |
PubChem ID | 58423153 |
InChI Key | MCUJKPPARUPFJM-UWCCDQBKSA-N |
Smiles | N[C@@H]1CCCN(C2=C(C3=CC=CC=C3)C=CC=C2/C=C4SC(NC\4=O)=O)C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 7.59 | 20 温和加热 |
以下数据基于产品分子量 379.48。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.2 mM | 13.18 mL | 65.88 mL | 131.76 mL |
1 mM | 2.64 mL | 13.18 mL | 26.35 mL |
2 mM | 1.32 mL | 6.59 mL | 13.18 mL |
10 mM | 0.26 mL | 1.32 mL | 2.64 mL |
参考文献是支持产品生物活性的出版物。
Keeton et al (2014) AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia. Blood 123 905 PMID: 24363397
Brasó-Maristany et al (2016) PIM1 kinase regulates cell death, tumor growth and chemotherapy response in triple-negative breast cancer. Nat.Med. 22 1303 PMID: 27775704
Dakin et al (2012) Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases. Bioorg.Med.Chem.Lett. 22 4599 PMID: 22727640
Salazar et al (2022) Targeting host PIM protein kinases reduces Mayaro virus replication. Viruses 14 422 PMID: 35216015
If you know of a relevant reference for AZD 1208, please let us know.
关键词: AZD 1208, AZD 1208 supplier, AZD1208, pan, Pim, kinase, 1, 2, 3, potent, active, in, vivo, anticancer, inhibitors, inhibits, chemosensitizer, antiviral, effects, against, Mayaro, virus, Kinase, Other, Antivirals, 6310, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 AZD 1208 的部分引用包括:
Salazar et al (2022) Targeting host PIM protein kinases reduces Mayaro virus replication. Viruses 14 422 PMID: 35216015
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