Hsp90-IN-48
Hsp90-IN-48 is an orally active Hsp90 inhibitor with an IC50 of 19.4 nM. Hsp90-IN-48 improves tumor-cell uptake and intracellular active-component release, and suppresses tumor metastasis. Hsp90-IN-48 induces G2/M phase cell cycle arrest and tumor cell apoptosis whlie simultaneously inhibits Top1/Top2 activity. Hsp90-IN-48 inhibits tumor growth and can be used for colon cancer research.
For research use only. We do not sell to patients.
- CAS No.: 3117528-53-4
- Formula: C45H43FN6O8
- Molecular Weight:814.86
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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
All Topoisomerase Isoforms
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Biological Activity
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HSP90 19.4 nM (IC50) |
Top1 |
Top2 |
Hsp90-IN-48 (compound 5a) (72 h) inhibits the proliferation of HCT116, MCF-7, and MIA PaCa-2 cells with IC50 values of 7.7 nM, 31.8 nM, and 10.7 nM, respectively, and exhibits reduced cytotoxicity against HUVEC cells with an IC50 of 74.2 nM[1].
Hsp90-IN-48 (50 nM, 100 nM) inhibits HCT116 cell invasion, with an invasion inhibition rate higher than 35% at 100 nM[1].
Hsp90-IN-48 (20-100 nM; 48 h) induces G2/M phase arrest and apoptosis in HCT116 cells[1].
Hsp90-IN-48 (1 μM; 3 h) shows high cellular uptake in HCT116 cells with lower uptake in HUVEC cells[1].
Hsp90-IN-48 exhibits good metabolic stability in mouse liver microsomes, with a t1/2 of 86.6 min and a CLint of 10.3 mL/min/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116
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Concentration:20, 50, 100 nM
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Incubation Time:48 h
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Result:Induced G2/M phase arrest in a concentration-dependent manner.
Increased the proportion of HCT116 cells in the G2/M phase to 48.86%, 83.06% and 88.34% at 20 nM, 50 nM and 100 nM, respectively, compared with 18.27% in the control group.
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Cell Line:HCT116
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Concentration:20, 50, 100 nM
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Incubation Time:48 h
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Result:Induced HCT116 cell apoptosis in a concentration-dependent manner.
Increased the apoptotic cell percentages to 18.45%, 25.85% and 43.92% at 20 nM, 50 nM and 100 nM, respectively, compared with 0.44% in the control group.
| Species | Dose | Route | T1/2 | AUC0-∞ | Vss | CL |
|---|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 0.22 h | 4313.79 ng·h/mL | 0.03 L/kg | 5.97 mL/min/kg |
Hsp90-IN-48 (12, 24 mg/kg; p.o.; once daily; for 15 consecutive days) has oral antitumor activity in HCT116 xenograft nude mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude mice subcutaneously implanted with HCT116 cells (about 5 × 106 cells) into the right axilla region[1]
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Dosage:6, 12 mg/kg
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Administration:Intraperitoneal injection (i.p.); once daily; for 21 consecutive days
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Result:Suppressed HCT116 xenograft tumor growth in a dose-dependent manner.
Achieved TGI values of 63.1% at 6 mg/kg and 72.9% at 12 mg/kg.
Reduced tumor volume and tumor weight compared with the vehicle group.
Did not cause obvious body weight loss during the 21-day dosing period.
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Animal Model:Female nude mice subcutaneously implanted with HCT116 cells (about 5 × 106 cells) into the right axilla region[1]
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Dosage:12, 24 mg/kg
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Administration:Oral gavage (p.o.); once daily; for 15 consecutive days
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Result:Suppressed HCT116 xenograft tumor growth after oral administration in a dose-dependent manner.
Achieved TGI values of 47.3% at 12 mg/kg and 61.2% at 24 mg/kg.
Reduced tumor volume and tumor weight compared with the vehicle group.
Did not cause obvious body weight changes during the 15-day dosing period.
Showed lowepathological toxicity in heart, liver, spleen, lung and kidney sections in H&E staining assay..
Reduced Ki67 expression and increased TUNEL signal in tumor sections, indicating reduced tumor cell proliferation and increased tumor cell apoptosis in vivo.
Chemical Information
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CAS No. 3117528-53-4
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Molecular Weight 814.86
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Formula C45H43FN6O8
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SMILES
OC(C(C(C)C)=C1)=CC(O)=C1C2=C(C3=CC=C(CN4CCOCC4)C=C3)C(C(NCC(OC5=CC=C(NC6=C7CCN8C6N(C)C(C=CC(F)=C9)=C9C8=O)C7=C5)=O)=O)=NO2
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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)
Hsp90-IN-48 Related Classifications
Cat. No.: HY-184245
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- Hsp90-IN-48
- 3117528-53-4
- HSP
- Topoisomerase
- Apoptosis
- Hsp90 inhibitor
- orally active
- evodiamine derivative conjugate
- eHsp90
- Top2 inhibitor
- Top1 inhibitor
- tumor-targeted uptake
- HCT116
- MCF-7
- MIA PaCa-2
- HUVEC
- G2/M arrest
- apoptosis
- cell invasion
- HCT116 xenograft model
- colon cancer
- oral administration
- intraperitoneal injection
- Inhibitor
- inhibitor
- inhibit