Antiproliferative agent-23
Antiproliferative agent-23 is a microtubule-destabilizing agent (MDA) and efficiently disturbes the tubulin-microtubule system. Antiproliferative agent-23 induces apoptosis via a mitochondrion-dependent pathway by downregulating the Bcl-2 protein, upregulating Bax and Cyt c proteins, and activating the caspase cascade. Antiproliferative agent-23 initiates reactive oxygen species (ROS)-mediated endoplasmic reticulum stress in A549/CDDP cells (cisplatin resistant cancer cell line) via the PERK/ATF4/CHOP signaling pathway. Antiproliferative agent-23 has anti-tumor activity.
For research use only. We do not sell to patients.
- CAS No.: 3049213-47-7
- Formula: C23H28Cl3N3O6Pt
- Molecular Weight:743.93
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Antiproliferative agent-23 (72 hours) has vitro antiproliferative effect in HepG2 (IC50=0.86), MDA-MB-231 (IC50=1.53), MCF-7 (IC50=0.94), A2780 (IC50=0.88), A549 (IC50=0.23), A549/CDDP (IC50=0.35), HepG2/CDDP (IC50=1.16), HUEVC (IC50=5.68)[1].
Antiproliferative agent-23 (5 μM; 24 hours) effectively induces cell apoptosis in A549/CDDP cells[1].
Antiproliferative agent-23 (5 μM; 24 hours) can efficiently cause DNA damage in A549/CDDP cells and thus ultimately triggered apoptosis. Antiproliferative agent-23 causes a significant increase in the ER stress-related protein expression[1].
Antiproliferative agent-23 (10, 20 μM; 24 hours) leads to inhibitory effects of polymerization with an IC50 of 9.86 μM[1].
Antiproliferative agent-23 (5 μM; 24 hours) significantly increases intracellular ROS in A549/CDDP cells[1].
Antiproliferative agent-23 (1 μM; 24 hours) potently inhibits A549 cell migration in in vitro assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CDDP-resistant non-small cell lung cancer cell line (A549/CDDP)
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Concentration:5 μM
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Incubation Time:24 hours
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Result:Effectively induced cell apoptosis in A549/CDDP cells.
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Cell Line:CDDP-resistant non-small cell lung cancer cell line (A549/CDDP)
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Concentration:5 μM
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Incubation Time:24 hours
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Result:Induced a high level of γ-H2AX.
Caused a significant increase in the ER stress-related protein (p-PERK, p-eIF2α, ATF 4, and CHOP) expression.
The level of Bcl-2 was downregulated.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c nude mice (20 to 25 g) injected with A549/CDDP[1]
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Dosage:12.40 mg/kg
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Administration:IV; every 7 days for 28 consecutive days
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Result:The tumor growth inhibition (TGI) values significantly increased to 65.9%.
Chemical Information
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CAS No. 3049213-47-7
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Molecular Weight 743.93
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Formula C23H28Cl3N3O6Pt
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SMILES
O=C(C1=CC(OC)=C(C(OC)=C1)OC)/C=C/C2=CC=CC3=C2C=CN3CCC(O[Pt](Cl)(Cl)(Cl)([NH3])[NH3])=O
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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
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Data Sheet (276 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- Antiproliferative agent-23
- 3049213-47-7
- Antiproliferative agent23
- Antiproliferative agent 23
- Microtubule/Tubulin
- Apoptosis
- microtubule-destabilizing agent
- MDA
- tubulin
- microtubule
- mitochondrion
- Bcl-2
- Bax
- Cyt c
- caspase cascade
- reactive oxygen species
- ROS
- endoplasmic reticulum stress
- A549/CDDP
- PERK
- ATF4
- CHOP
- anti-tumor
- Inhibitor
- inhibitor
- inhibit