2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
  3. Topoisomerase HSP Apoptosis
  4. 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.

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Hsp90-IN-48

Hsp90-IN-48 Chemical Structure

CAS No. : 3117528-53-4

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Hsp90-IN-48 Related Antibodies

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Description

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[1].

IC50 & Target[1]

HSP90

19.4 nM (IC50)

Top1

 

Top2

 

In Vitro

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.

Hsp90-IN-48 Related Antibodies

Cell Cycle Analysis

Cell Line: HCT116
Concentration: 20, 50, 100 nM
Incubation Time: 48 h
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.

Apoptosis Analysis

Cell Line: HCT116
Concentration: 20, 50, 100 nM
Incubation Time: 48 h
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.
Parmacokinetics
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
In Vivo

Hsp90-IN-48 (Compound 5a) (6, 12 mg/kg; i.p.; once daily; for 21 consecutive days) has antitumor activity in HCT116 xenograft nude mouse model[1].
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.

Animal Model: Female nude mice subcutaneously implanted with HCT116 cells (about 5 × 106 cells) into the right axilla region[1]
Dosage: 6, 12 mg/kg
Administration: Intraperitoneal injection (i.p.); once daily; for 21 consecutive days
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.
Animal Model: Female nude mice subcutaneously implanted with HCT116 cells (about 5 × 106 cells) into the right axilla region[1]
Dosage: 12, 24 mg/kg
Administration: Oral gavage (p.o.); once daily; for 15 consecutive days
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.
Molecular Weight

814.86

Formula

C45H43FN6O8
CAS No.
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
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
References
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Hsp90-IN-48 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Hsp90-IN-483117528-53-4TopoisomeraseHSPApoptosisHeat shock proteinsHsp90 inhibitororally activeevodiamine derivative conjugateeHsp90Top2 inhibitorTop1 inhibitortumor-targeted uptakeHCT116MCF-7MIA PaCa-2HUVECG2/M arrestapoptosiscell invasionHCT116 xenograft modelcolon canceroral administrationintraperitoneal injectionInhibitorinhibitorinhibit

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