STA-1474 sodium
STA-1474 sodium is an orally active and highly selective HSP90 inhibitor, as well as a phosphate prodrug of the HSP90 inhibitor STA-9090 (HY-15205). STA-1474 sodium disrupts the chaperone function of HSP90 and promotes the degradation of client proteins. STA-1474 sodium inhibits the phosphorylation of Met, Akt and STAT3, thereby blocking related signaling pathways. STA-1474 sodium induces apoptosis and inhibits proliferation of osteosarcoma cells, and triggers the up-regulation of HSP70 and HSP90. STA-1474 sodium induces tumor regression and caspase-3 activation in mouse osteosarcoma xenograft models. STA-1474 sodium can be used in the research of osteosarcoma.
For research use only. We do not sell to patients.
- CAS No.: 1402907-09-8
- Formula: C20H19N4Na2O6P
- Molecular Weight:488.34
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Caspase Isoforms
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Biological Activity
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HSP90 |
HSP70 |
Caspase 3 |
p-STAT3 |
Met |
Akt |
STA-1474 (0.001-1 μM; 1-7 days) sodium potently inhibits the proliferation of D17, OSA2, OSA8 and MG63 osteosarcoma cell lines, with IC50 values ranging from 0.011 μM to 0.043 μM, and exhibits selectivity for OSA cells relative to normal canine osteoblasts (IC50 = 0.072 μM)[1].
STA-1474 (0.1 μM; 24-48 h, followed by drug-free incubation for 2-6 h) sodium mediates time-dependent and reversible downregulation of p-STAT3 in MG63 and D17 osteosarcoma cell lines, which confirms that this effect directly results from HSP90 inhibition rather than non-specific toxicity[1].
STA-1474 (0.01-1 μM; 24-48 h) sodium induces dose-dependent apoptosis in OSA8 and MG63 osteosarcoma cell lines, but does not affect apoptosis in normal canine osteoblasts; it activates caspase 3/7 in a dose-dependent manner in D17 and OSA8 osteosarcoma cell lines, and induces dose-dependent PARP cleavage in D17, OSA2, OSA8 and MG63 osteosarcoma cell lines; it downregulates HSP90 client proteins (p-Met, total Met, p-Akt, total Akt, p-STAT3), and induces upregulation of stress response proteins HSP70 and HSP90[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1402907-09-8
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Molecular Weight 488.34
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Formula C20H19N4Na2O6P
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SMILES
O=C1NN=C(N1C2=CC(C=CN3C)=C3C=C2)C4=C(O)C=C(OP(O[Na])(O[Na])=O)C(C(C)C)=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)