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Onalespib

Chemical Structure : Onalespib

CAS No.: 912999-49-6

Onalespib (AT13387, AT-13387)

Catalog No.: PC-25124Not For Human Use, Lab Use Only.

Onalespib (AT13387) is a highly potent HSP90 inhibitor with Ki of 0.71 nM by binding in the ATPase site at the N-terminus of Hsp90, inhibits HCT116 cell proliferation with IC50 of 48 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Onalespib (AT13387) is a highly potent HSP90 inhibitor with Ki of 0.71 nM by binding in the ATPase site at the N-terminus of Hsp90, inhibits HCT116 cell proliferation with IC50 of 48 nM.
Onalespib (AT13387) potently inhibits the expression of the oncogenic client proteins Raf-1 and CDK4 at 30 nM in the HCT116 cell line.
Onalespib (AT13387) potently inhibits the proliferation of a panel of human tumor cell lines (well over 100 cell lines have been tested), showing IC50 < 100 nM.
Onalespib (AT13387) (60 mg/kg ip 3 days on and 3 days off for four cycles) exhibits in vivo antitumor activity in nude BALB/c mice bearing early stage HCT116 human colon carcinoma xenografts.

Physicochemical Properties

M.Wt 409.53
Formula C24H31N3O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2,4-Dihydroxy-5-isopropylphenyl)(5-((4-methylpiperazin-1-yl)methyl)isoindolin-2-yl)methanone

References

1. Woodhead AJ, et al. J Med Chem. 2010 Aug 26;53(16):5956-69.

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