HSP-990 Inhibitor CAS No. 934343-74-5

Cat. No.	Name	Size	Price
KI1485	HSP-990	10 mg	$530
	HSP-990	50 mg	$620
	HSP-990	50 mg	$736

Chemical Characteristic

Product Name	HSP-990
Synonyms	NVP-HSP990
CAS No.	934343-74-5
Molecular Weight	379.39
Formula	C₂₀H₁₈FN₅O₂
Chemical Name	(7R)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one
Smiles	c1(nc2c(c(n1)C)C(=O)N[C@H](C2)c1c(cc(cc1)F)c1cccc(n1)OC)N
Chemical Structure
Documents	CNMR HNMR HPLC LCMS

Biological activities

HSP-990 is an potent inhibitor of human heat-shock protein 90 (Hsp90). The IC50 values of HSP-990 against four of the Hsp90 isoforms Hsp90α, Hsp90β, GRP94 and TRAP-1 are 0.6, 0.8, 8.5, and 320 nM, respectively. In c-Met amplified GTL-16 gastric tumor cells, HSP-990 dissociates the Hsp90-p23 complex, depletes client protein c-Met, and induces Hsp70 in vitro. HSP-990 also potently inhibits the growth of human cell lines including GTL-16, N87, MV4, and HCT116 in vitro.^[1]HSP-990 binds with high affinity to the N-terminal ATP binding pocket of HSP90. HSP-990 potently reduces viability in a time- and dose-dependent manner in multiple myeloma cell lines. HSP-990 effectively induces apoptosis, in part via caspase activation. HSP-990 also leads to a significant reduction in induced G2 cell cycle arrest and degradation of caspase-8 and caspase-3 in myeloma cell. In addition, combined incubation with melphalan and HSP-990 leads to synergistically increased cleavage of caspase-2, caspase-9, and caspase-3.^[2] In the GTL-16 xenograft model, a single oral administration of 15 mg/kg of HSP-990 induces sustained downregulation of c-Met and upregulation of Hsp70. In repeat dosing studies, HSP-990 treatment results in tumor growth inhibition of GTL-16 tumor xenograft models driven by well-defined oncogenic Hsp90 client proteins.^[1]

Protocols

In vitro: HSP-990 is dissolved in DMSO.^[3]

References

[1] Menezes DL, et al. The novel oral Hsp90 inhibitor NVP-HSP990 exhibits potent and broad-spectrum antitumor activities in vitro and in vivo. Mol Cancer Ther. 2012, 11(3): 730-739. [2] Lamottke B, et al. The novel, orally bioavailable HSP89 inhibitor NVP-HSP990 induces cell cycle arrest and apoptosis in multiple myeloma cells and acts synergistically with melphalan by increased cleavage of caspases. Eur J Haematol. 2012, 88(5): 406-415. [3] Centenera MM, et al. Evidence for efficacy of new Hsp90 inhibitors revealed by ex vivo culture of human prostate tumors. Clin Cancer Res. 2012, 18(13): 3562-3570.

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