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Cat. No.: HY-13752B

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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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Please store the product under the recommended conditions in the Certificate of Analysis.

STA-1474 sodium Chemical Structure

CAS No.: 1402907-09-8

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
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Biological Activity

Description

IC₅₀ & Target

^[1]

HSP90

HSP70

Caspase 3

p-STAT3

Met

Akt

All HSP Isoforms :

All Caspase Isoforms :

All STAT Isoforms :

All Akt Isoforms :

In Vitro

Anti-cancerApoptosis

Anti-cancer

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].

Anti-cancer

Apoptosis

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.

In Vivo

Anti-cancerApoptosis

Anti-cancer

Apoptosis

STA-1474 (60 mg/kg; intravenous injection; three times per week for 2 weeks) sodium exhibits potent in vivo anti-osteosarcoma activity, and induces apoptosis and downregulation of client proteins^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Related Protocols :

Chemical Information

CAS No. 1402907-09-8
Molecular Weight 488.34
Formula C₂₀H₁₉N₄Na₂O₆P
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. McCleese JK, et al. The novel HSP90 inhibitor STA-1474 exhibits biologic activity against osteosarcoma cell lines. International journal of cancer. 2009 Dec 15;125(12):2792-801. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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STA-1474 sodium

All HSP Isoforms

All Caspase Isoforms

All STAT Isoforms

All Akt Isoforms