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Product Description
– AZD4877 is another isostere to Ispinesib (HY-50759)and also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. AZD4877 inhibits circulating peripheral blood mononuclear cells (PBMCs) and has anti-cancer activity[1][2][3][4][5].
Web ID
– HY-13224
Shipping
– Room temperature
Applications
– Cancer-programmed cell death
Molecular Formula
– C28H33N5O2S
References
– [1]Shahin R, et.al. Kinesin spindle protein inhibitors in cancer: from high throughput screening to novel therapeutic strategies. Future Sci OA. 2022 Feb 21;8(3):FSO778. |[2]Myers SM, et.al. Recent findings and future directions for interpolar mitotic kinesin inhibitors in cancer therapy. Future Med Chem. 2016;8(4):463-89. |[3]Theoclitou ME, et.al. Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent. J Med Chem. 2011 Oct 13;54(19):6734-50. |[4]Marquis L, et.al. p63 expression correlates with sensitivity to the Eg5 inhibitor ZD4877 in bladder cancer cells. Cancer Biol Ther. 2012 May;13(7):477-86. |[5]Gerecitano JF, et.al. A Phase I trial of the kinesin spindle protein (Eg5) inhibitor AZD4877 in patients with solid and lymphoid malignancies. Invest New Drugs. 2013 Apr;31(2):355-62.
CAS Number
– 758722-49-5
Molecular Weight
– 503.66
SMILES
– O=C(N(C(C(C)C)C1=NC2=C(C(N1CC3=CC=CC=C3)=O)C(C)=NS2)CCCN)C4=CC=C(C)C=C4
Clinical Information
– Phase 2
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– Apoptosis;Kinesin
Pathway
– Apoptosis;Cell Cycle/DNA Damage;Cytoskeleton
Product type
– Reference compound
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