CHNQD-01522
CHNQD-01522 is a microtubule inhibitor targeting the colchicine binding site on β-tubulin. CHNQD-01522 binds to the colchicine binding site on β-tubulin, inhibits microtubule polymerization, and evades P-glycoprotein transport in cancer cells. CHNQD-01522 inhibits proliferation, suppresses tumor cell colony formation, arrests cell cycle in G2/M phases, and induces apoptosis in cancer cells. CHNQD-01522 upregulates of Bax and activation of caspase-9 and caspase-3. CHNQD-01522 shows anti-tumor efficacy in subcutaneous and orthotopic hepatocellular carcinoma xenograft tumor models. CHNQD-01522 can be used for the research of hepatocellular carcinoma.
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- Fòrmula: C19H18N2O5
- Peso molecular:354.36
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Bax |
Caspase 3 |
Caspase-9 |
CHNQD-01522 (Compound 18) (72 h) potently inhibits proliferation of Huh-7, Hep G2, A549, HT-29, U251, and BT-549 cells with IC50 values of 0.17-0.3 μM, and exhibits favorable selectivity for cancer cells over normal L-02 liver cells[1].
CHNQD-01522 (0.125-0.25 μM; 5 days) dose-dependently inhibits colony formation of Huh-7 cells, with near-complete inhibition at 0.25 μM over 5 days[1].
CHNQD-01522 (0.125-0.25 μM; 24 h) induces G2/M phase cell cycle arrest in Huh-7 cells, with a marked increase in G2/M phase cells at 0.25 μM after 24 h[1].
CHNQD-01522 (0.125-0.25 μM; 24 h) induces significant apoptosis in Huh-7 cells, with a marked increase in total apoptotic cells at 0.25 μM after 24 h[1].
CHNQD-01522 (0.125-0.5 μM; 24 h) activates the mitochondrial intrinsic apoptotic pathway in Huh-7 cells via dose-dependent upregulation of Bax and activation of caspase-9 and caspase-3 after 24 h of treatment[1].
CHNQD-01522 (10-20 μM; 90 min) dose-dependently inhibits tubulin polymerization, acting as a microtubule-destabilizing agent[1].
CHNQD-01522 (0.125-0.25 μM; 6 h) disrupts the microtubule cytoskeleton organization in Huh-7 cells after 6 h of treatment at 0.125 μM and 0.25 μM[1].
CHNQD-01522 (10-100 μM; 1 h) directly interacts with β-tubulin in Huh-7 cell lysates, increasing its stability against proteolytic digestion[1].
CHNQD-01522 (10-100 μM; 2 h) competes with EBI for the colchicine binding site on β-tubulin in Huh-7 cells[1].
CHNQD-01522 is not a substrate of P-gp and does not modulate P-gp efflux function, indicating inherent resistance to P-gp-mediated multidrug resistance[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Huh-7
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Concentration:0.125 μM, 0.25 μM
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Incubation Time:24 h
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Result:Increased the proportion of G2/M phase-arrested cells.
Reduced the proportion of G1 phase-arrested cells.
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Cell Line:Huh-7
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Concentration:0.125 μM, 0.25 μM
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Incubation Time:24 h
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Result:Raised the total apoptotic cell population from 2.51% (control) to 31.84% at 0.25 μM.
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Cell Line:Huh-7
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Concentration:0.125 μM, 0.25 μM, 0.5 μM
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Incubation Time:24 h
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Result:Upregulated Bax expression in a dose-dependent manner.
Activated caspase-9 and caspase-3 in a dose-dependent manner.
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Cell Line:Huh-7
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Concentration:0.125 μM, 0.25 μM
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Incubation Time:6 h
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Result:Induced marked disruption of the microtubule cytoskeleton, with structural alterations similar to those caused by vincristine.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | MRT0-t | F | C0 |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 2.5 mg/kg | i.v. | 0.336 h | 0.083 h | 6140.244 ng/mL | 3180.121 ng·h/mL | 0.356 h | 100 % | 7515.850 ng/mL |
| Rat[1] | 10 mg/kg | i.p. | 1.326 h | 0.083 h | 12122.205 ng/mL | 11041.089 ng·h/mL | 1.097 h | 86.8 % | / |
| Rat[1] | 30 mg/kg | p.o. | 8.421 h | 0.25 h | 822.671 ng/mL | 3325.864 ng·h/mL | 14.011 h | 8.715 % | / |
CHNQD-01522 (1 mg/kg; i.p.; three times daily (TID); 14 days) significantly reduces tumor volume in an Huh-7 orthotopic hepatocellular carcinoma xenograft model, with no observed body weight loss[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c-nu (female, 6-7 weeks old, 14 ± 1 g, Huh‑7 subcutaneous xenograft model)[1]
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Dosage:2 mg/kg
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Administration:i.p.; QD/BID/TID; 14 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 70.22% for tumor volume and 79.09% for tumor weight with 2 mg/kg TID regimen.
Delayed tumor progression in a dosing frequency-dependent manner.
Caused no significant body weight changes or adverse effects in any treated groups.
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Animal Model:BALB/c-nu (female, 6-7 weeks old, 14 ± 1 g, Huh‑7 orthotopic xenograft model)[1]
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Dosage:1 mg/kg
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Administration:i.p.; TID; 14 days
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Result:Resulted in a statistically significant reduction in tumor volume compared to the control group.
Caused no notable body weight changes in the treatment group.
Chemical Information
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Peso molecular 354.36
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Fòrmula C19H18N2O5
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SMILES
COC1=CC(C(C(N2)=NC3=CC(C)=CC=C3C2=O)=O)=CC(OC)=C1OC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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