1160952-43-1

Name	[1,1'-Biphenyl]-3-carboxamide, N-[7-(acetyloxy)-8-methoxy-2-oxo-2H-1-benzopyran-3-yl]-3',6-dimethoxy-
CAS	1160952-43-1
Molecular Formula	C27H23NO8
Molecular Weight	489.47
MOL File	1160952-43-1.mol

Synonyms

KU-177 [1,1'-Biphenyl]-3-carboxamide, N-[7-(acetyloxy)-8-methoxy-2-oxo-2H-1-benzopyran-3-yl]-3',6-dimethoxy-

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Chemical Properties

Boiling point	714.9±60.0 °C(Predicted)
density	1.37±0.1 g/cm3(Predicted)
pka	7.58±0.20(Predicted)

Hazard Information

Uses

KU-177 is a potent inhibitor of Hsp90 ATPase homologue 1 (Aha1), ablates Aha1-driven enhancement of Hsp90-dependent tau aggregation. KU-177 also disrupts Aha1/Hsp90 interactions (IC50=4.08 μM) without inhibition of Hsp90’s ATPase activity. KU-177 can be used for tauopathies research[1][2].

in vivo

KU-177 (1 mg/kg; i.p.; twice a week; 4 weeks), inhibits tumor growth and extends the survival of 5TMM3VT MM mice without significant toxicity. KU-177 shows stronger efficacy in vivo, combined with Bortezomib.html" class="link-product" target="_blank">Bortezomib (HY-10227) (1 mg/kg; i.p.)^[1].

Animal Model:	5TMM3VT mouse model (6-8 weeks old, C57BL/KaLwrij mice)^[1]
Dosage:	1 mg/kg
Administration:	Intraperitoneal injection; twice a week; sacrificed mice with hindlimb weakness immediately, about 4-5 weeks
Result:	Inhibited the xenograft tumor growth of both ANBL6 WT/BTZ-DR cells. Didn’t induce histopathological abnormities or lesions in main organs including heart, liver, spleen, lung and kidney.

IC 50

HSP90

References

[1] Gu C, et al. AHSA1 is a promising therapeutic target for cellular proliferation and proteasome inhibitor resistance in multiple myeloma. J Exp Clin Cancer Res. 2022 Jan 6;41(1):11. DOI:10.1186/s13046-021-02220-1
[2] Keegan BM, et al. Synthesis and Evaluation of Small Molecule Disruptors of the Aha1/Hsp90 Complex for the Reduction of Tau Aggregation. ACS Med Chem Lett. 2022 Apr 15;13(5):827-832. DOI:10.1021/acsmedchemlett.2c00064

Spectrum Detail

[1,1'-Biphenyl]-3-carboxamide, N-[7-(acetyloxy)-8-methoxy-2-oxo-2H-1-benzopyran-3-yl]-3',6-dimethoxy-(1160952-43-1)¹HNMR

Supplier

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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