Benzamide, N-(3-aminopropyl)-N-[1-[4,5-dihydro-3-methyl-4-oxo-5-(phenylmethyl)isothiazolo[5,4-d]pyrimidin-6-yl]-2-methylpropyl]-4-methyl-

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Benzamide, N-(3-aminopropyl)-N-[1-[4,5-dihydro-3-methyl-4-oxo-5-(phenylmethyl)isothiazolo[5,4-d]pyrimidin-6-yl]-2-methylpropyl]-4-methyl- Basic information
Product Name:Benzamide, N-(3-aminopropyl)-N-[1-[4,5-dihydro-3-methyl-4-oxo-5-(phenylmethyl)isothiazolo[5,4-d]pyrimidin-6-yl]-2-methylpropyl]-4-methyl-
Synonyms:Benzamide, N-(3-aminopropyl)-N-[1-[4,5-dihydro-3-methyl-4-oxo-5-(phenylmethyl)isothiazolo[5,4-d]pyrimidin-6-yl]-2-methylpropyl]-4-methyl-;N-(3-Aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydroisothiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide
CAS:758722-49-5
MF:C28H33N5O2S
MW:503.66
EINECS:
Product Categories:
Mol File:758722-49-5.mol
Benzamide, N-(3-aminopropyl)-N-[1-[4,5-dihydro-3-methyl-4-oxo-5-(phenylmethyl)isothiazolo[5,4-d]pyrimidin-6-yl]-2-methylpropyl]-4-methyl- Structure
Benzamide, N-(3-aminopropyl)-N-[1-[4,5-dihydro-3-methyl-4-oxo-5-(phenylmethyl)isothiazolo[5,4-d]pyrimidin-6-yl]-2-methylpropyl]-4-methyl- Chemical Properties
form Solid
color Off-white to light yellow
Safety Information
MSDS Information
Benzamide, N-(3-aminopropyl)-N-[1-[4,5-dihydro-3-methyl-4-oxo-5-(phenylmethyl)isothiazolo[5,4-d]pyrimidin-6-yl]-2-methylpropyl]-4-methyl- Usage And Synthesis
UsesAZD4877 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].
in vivo

AZD4877 (i.v., 6 mg/kg, 12 mg/kg; single dose) has a significant reduction in cell viability and increase in cleaved caspase 3 levels by 48 h post dose in a rat hollow fiber model[1].
AZD4877 (i.v., 6 mg/kg; single dose) shows a T1/2 of 3.5 h, and CL of 36 mL/min/kg in Hans Wistar rats[1].

References[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. DOI:10.1021/jm200629m
[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. DOI:10.4161/cbt.19590
[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. DOI:10.1007/s10637-012-9821-y
[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. DOI:10.2144/fsoa-2021-0116
[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. DOI:10.4155/fmc.16.5
Benzamide, N-(3-aminopropyl)-N-[1-[4,5-dihydro-3-methyl-4-oxo-5-(phenylmethyl)isothiazolo[5,4-d]pyrimidin-6-yl]-2-methylpropyl]-4-methyl- Preparation Products And Raw materials
Tag:Benzamide, N-(3-aminopropyl)-N-[1-[4,5-dihydro-3-methyl-4-oxo-5-(phenylmethyl)isothiazolo[5,4-d]pyrimidin-6-yl]-2-methylpropyl]-4-methyl-(758722-49-5) Related Product Information
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