GN-604
GN-604 is a targeted drug conjugate (Targeted Drug Conjugate, TDC) formed by conjugation of GNS561 (HY-137978) with DN604, a Pt (II) complex. GN-604 selectively inhibits PPT1, induces lysosomal dysfunction, suppresses autophagy and triggers apoptosis. GN-604 promotes the targeted sequestration of Pt (II) inside cells, induces DNA damage and inhibits the proliferation of malignant cells. GN-604 is applicable to research related to triple-negative breast cancer.
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- Formule: C31H37ClN8O6Pt
- Masse moléculaire:848.21
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
GN-604 (72 h) inhibits proliferation of HUH-7, HepG2, HT-29, MDA-MB-231, A549, and CDDP (HY-17394)-resistant A549/CDDP cancer cells with IC50 values ranging from 5.32 μM to 9.03 μM, and shows high tumor selectivity with low toxicity to HUVEC cells (IC50 = 29.56 μM) and potential to overcome CDDP resistance[1].
GN-604 (10 μM; 24 h) inhibits MDA-MB-231 cell migration more effectively than CDDP or GNS561 alone, with a migration rate of 37.4%[1].
GN-604 (10-20 μM; 2 weeks) inhibits MDA-MB-231 cell colony formation in a dose-dependent manner, with greater efficacy at 20 μM than at 10 μM[1].
GN-604 (10-20 μM; 24 h) induces apoptosis in MDA-MB-231 cells in a dose-dependent manner, with an apoptotic rate of 15.8% at 10 μM and 33.6% at 20 μM[1].
GN-604 (10 μM; 24 h) induces S phase arrest in MDA-MB-231 cells[1].
GN-604 (10 μM; 24 h) downregulates PPT1 expression and increases LC3B-II levels in MDA-MB-231 cells, disrupting lysosomal function and inhibiting autophagic flux[1].
GN-604 (10 μM; 24 h) upregulates γ-H2AX expression in MDA-MB-231 cells, indicating induction of DNA double-strand breaks[1].
GN-604 (10 μM; 12 h) induces lysosomal dysfunction in MDA-MB-231 cells, as evidenced by increased LysoTracker Red fluorescence intensity and enlarged lysosome size[1].
GN-604 (10 μM; 12 h) disrupts lysosomal acidification in MDA-MB-231 cells, as shown by altered Acridine Orange fluorescence ratios[1].
GN-604 (0.25 μM; 12 h) achieves 1.8-fold higher intracellular platinum accumulation in MDA-MB-231 cells than CDDP at the same concentration[1].
GN-604 (10-20 μM; 12 h) induces DNA strand breaks in MDA-MB-231 cells in a dose-dependent manner, with greater damage observed at 20 μM than at 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231
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Concentration:10 μM
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Incubation Time:24 h
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Result:Limited MDA-MB-231 cell migration to a rate of 37.4%, which was more potent than standalone CDDP (43.6%) or GNS561 (41.2%), but slightly less potent than the GNS561+CDDP combination (28.3%).
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Cell Line:MDA-MB-231
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Concentration:10-20 μM
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Incubation Time:24 h, followed by ~2 weeks of drug-free incubation
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Result:Inhibited colony formation in a dose-dependent manner, with efficacy equivalent to GNS561 at 10 μM and stronger inhibition at 20 μM, though slightly less potent than the GNS561+CDDP combination.
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Cell Line:MDA-MB-231
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Concentration:10-20 μM
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Incubation Time:24 h
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Result:Induced apoptosis in MDA-MB-231 cells in a concentration-dependent manner: 10 μM resulted in 15.8% apoptotic cells, which was higher than CDDP (11.8%) and GNS561 (14.9%); 20 μM resulted in 33.6% apoptotic cells, comparable to the GNS561+CDDP combination (38.6%).
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Cell Line:MDA-MB-231
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Concentration:10 μM
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Incubation Time:24 h
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Result:Induced marked S phase arrest in MDA-MB-231 cells, increasing the proportion of cells in S phase compared to the control group.
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Cell Line:MDA-MB-231
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Concentration:10 μM
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Incubation Time:24 h
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Result:Significantly reduced PPT1 expression and increased LC3B-II levels, indicating impaired autophagic flux and lysosomal dysfunction.\nUpregulated γ-H2AX expression, inducing more pronounced DNA damage than CDDP alone, though slightly less than the GNS561+CDDP combination.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 5 weeks old, 16-18 g)[1]
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Dosage:14.0 mg/kg; 28.0 mg/kg
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Administration:i.v.; once a week; 24 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 63.65% at 14.0 mg/kg.
Increased the TGI rate to 72.88% at 28.0 mg/kg, which was higher than the TGI of the GNS561 + CDDP combination group.
Caused no significant body weight loss over the 24-day period.
Showed no obvious abnormalities in histopathological analysis of major organs (heart, liver, spleen, lung, kidney).
Induced pronounced morphological alterations including cellular deformation, necrosis, and nuclear fragmentation in tumor tissues at 28.0 mg/kg.
Upregulated γ-H2AX (a DNA damage marker) substantially and downregulated PPT1 expression pronouncedly in tumor tissues, with effects increasing with dose.
Chemical Information
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Masse moléculaire 848.21
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Formule C31H37ClN8O6Pt
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SMILES
ClC(C=C1)=CC=C1CNC2=NC3=CC=CC=C3C(N4CCC(NC(CCC(N/N=C5CC(C([O-][Pt+2]([NH3])([NH3])[O-]6)=O)(C6=O)C/5)=O)=O)CC4)=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GN-604 Related Classifications
HY-183351 Related Classifications
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