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AZD4877

AZD4877 is another isostere to Ispinesib 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].

Product Specifications

CAS Number

758722-49-5

UNSPSC

12352005

Target

Apoptosis; Kinesin; Mitosis

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Cytoskeleton

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/azd4877.html

Purity

99.49

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C)

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

Molecular Formula

C28H33N5O2S

Molecular Weight

503.66

References & Citations

[1]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. |[2]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. |[3]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. |[4]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. |[5]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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Available Sizes

Frequently Asked Questions

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