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STA-1474

Chemical Structure : STA-1474

CAS No.: 1118915-78-8

STA-1474 (STA1474)

Catalog No.: PC-20709Not For Human Use, Lab Use Only.

STA-1474 is a water soluble prodrug of Ganetespib (STA 9090), which is a potent, second generation small-molecule inhibitor of HSP90 (IC50=4 nM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

STA-1474 is a water soluble prodrug of Ganetespib (STA 9090), which is a potent, second generation small-molecule inhibitor of HSP90 (IC50=4 nM).
STA-1474 promoted loss of cell viability, inhibition of cell proliferation and induction of apoptosis in osteosarcoma (OSA) cell lines.
STA-1474 and its active metabolite STA-9090 also demonstrated increased potency compared to 17-AAG.
STA-1474 exhibited selectivity for OSA cells versus normal canine osteoblasts, and HSP90 co-precipitated with co-chaperones p23 and Hop in canine OSA cells but not in normal canine osteoblasts.
STA-1474 downregulated the expression of p-Met/Met, p-Akt/Akt and p-STAT3.
STA-1474 induced tumor regression, caspase-3 activation and downregulation of p-Met/Met and p-Akt/Akt in OSA xenografts.

Physicochemical Properties

M.Wt 444.38
Formula C20H21N4O6P
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

O=C1NN=C(C2=CC(C(C)C)=C(OP(O)(O)=O)C=C2O)N1C3=CC4=C(N(C)C=C4)C=C3

References

1. Lin TY, et al. Exp Hematol. 2008 Oct;36(10):1266-77.

2. McCleese JK, et al. Int J Cancer. 2009 Dec 15;125(12):2792-801.

3. Bansal H, et al. Blood. 2010 Nov 25;116(22):4591-9.

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