PF-4942847
PF-4942847 is an orally active HSP90 inhibitor with an IC50 of approximately 50 nM. PF-4942847 induces apoptosis in osteosarcoma cells, increases the proportion of cells in the sub-G1 phase and PARP cleavage, reduces the expression of Akt, Erk, MYC, c-MET and STAT-3, and regulates HSP expression. PF-4942847 can be used in studies related to osteosarcoma and HSP90.
For research use only. We do not sell to patients.
- CAS No.: 1046859-34-0
- Formula: C20H18Cl2F3N7O2
- Molecular Weight:516.31
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1299 | IC50 |
0.12 μM
Compound: 34
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Inhibition of human HSP90 in human NCI-H1299 cells assessed as Akt degradation after 24 hrs by luminex assay
Inhibition of human HSP90 in human NCI-H1299 cells assessed as Akt degradation after 24 hrs by luminex assay
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[PMID: 21438541] |
In Vitro
PF-4942847 inhibits cell growth in a dose-dependent manner in osteosarcoma cell lines U2OS, SaOS2, MNNG/HOS, KHOS, MG63, G292, CAL72, SJSA1 and 143B, with an IC50 of approximately 50 nM[1].
PF-4942847 induces apoptosis in osteosarcoma cell lines including U2OS, SaOS2, MNNG/HOS, KHOS, MG63, G292, CAL72, SJSA1 and 143B, as evidenced by increased proportions of cells in the sub-G1 phase and enhanced PARP cleavage[1].
PF-04942847 decreases the expression of Akt, Erk, MYC, c-MET and STAT-3, and modulates the expression of HSP in osteosarcoma cells[1].
PF-4942847 inhibits osteoclast differentiation of purified human CD14+ monocytes, and its effect differs from that of the control HSP90 inhibitor 17-AAG[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic mice bearing MNNG/HOS osteosarcoma xenografts[1]
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Dosage:25 mg/kg
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Administration:Oral administration (p.o.); 3 times/week
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Result:Significantly inhibited tumor growth by approximately 40% and prolonged survival compared with controls.
Chemical Information
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CAS No. 1046859-34-0
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Molecular Weight 516.31
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Formula C20H18Cl2F3N7O2
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SMILES
O=C(NCC(F)(F)F)N1CC=2N=C(N=C(C=3C(Cl)=CC(Cl)=CC3OCCN4N=CC=C4)C2C1)N
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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)
PF-4942847 Related Classifications
HY-108336 Related Classifications
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