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NVP-HSP990

Chemical Structure : NVP-HSP990

CAS No.: 934343-74-5

NVP-HSP990 (HSP990)

Catalog No.: PC-21200Not For Human Use, Lab Use Only.

NVP-HSP990 (HSP990) is a potent, selective, oral and brain-penetrant Hsp90 inhibitor with IC50 of 0.6, 0.8 and 8.5 nM for Hsp90α, Hsp90β and Grp94, respectively.

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

Biological Activity

NVP-HSP990 (HSP990) is a potent, selective, oral and brain-penetrant Hsp90 inhibitor with IC50 of 0.6, 0.8 and 8.5 nM for Hsp90α, Hsp90β and Grp94, respectively.
NVP-HSP990 inhibits TRAP1 ATPase activity with IC50 of 320 nM, binds to the N-terminal ATP-binding domain of Hsp90.
NVP-HSP990 does not show significant binding or functional activities against a panel of 83 diverse receptors/enzymes involved in major physiologic functions.
NVP-HSP990 induces a signature response of Hsp90 inhibition and inhibits growth of a wide range of tumor cells.
NVP-HSP990 (5 mg/kg twice weekly or 15 mg/kg weekly) demonstrates antitumor efficacy in the GTL-16 gastric cancer model.

Physicochemical Properties

M.Wt 379.40
Formula C20H18FN5O2
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

(7R)-2-amino-7-[4-fluoro-2-(6-methoxy-2-pyridinyl)phenyl]-7,8-dihydro-4-methyl-pyrido[4,3-d]pyrimidin-5(6H)-one

References

1. Centenera MM, et al. Clin Cancer Res. 2012 Jul 1;18(13):3562-70.

2. Menezes DL, et al. Mol Cancer Ther. 2012 Mar;11(3):730-9.

3. Jackrel ME, et al. J Clin Invest. 2011 Aug;121(8):2972-5.

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