Tubulin/PARP1-IN-1
Tubulin/PARP1-IN-1 is a dual inhibitor of tubulin and PARP1, with IC50 values of 1.86 μM and 0.88 μM, respectively. Tubulin/PARP1-IN-1 arrests cancer cells at the G2/M phase, induces cancer cell apoptosis, enhances cellular DNA damage, inhibits tumor angiogenesis, reduces cancer cell colonization and dissemination, and exhibits antiproliferative activity against colorectal cancer cells. Tubulin/PARP1-IN-1 can be used in the research of colorectal cancer and colorectal cancer lung metastasis.
For research use only. We do not sell to patients.
- Formula: C30H24Br2N4O6
- Molecular Weight:696.34
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Storage:
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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Biological Activity
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Chemical Information
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Biological Activity
Description
IC50 & Target
[1]|
PARP-1 0.88 μM (IC50) |
In Vitro
Tubulin/PARP1-IN-1 (Compound C2R) (72 h) exhibits inhibitory activity against HT-29, MCF-7, A549, PC-3, and MDA-MB-231, with an IC50 of 44 nM against HT-29[1].
Tubulin/PARP1-IN-1 (20-80 nM; 14 d) inhibits the number and size of HT-29 cell colonies in a dose-dependent manner[1].
Tubulin/PARP1-IN-1 (20-80 nM; 24 h) arrests HT-29 cells at the G2/M phase and induces apoptosis[1].
Tubulin/PARP1-IN-1 (40-80 nM; 24 h) reduces mitochondrial membrane potential and increases ROS levels in a dose-dependent manner in HT-29 cells[1].
Tubulin/PARP1-IN-1 (40-80 nM; 8 h) disrupts the microtubule network in HT-29 cells[1].
Tubulin/PARP1-IN-1 (20-40 nM; 24 h) significantly inhibits the invasion/migration capacity of A549 cells[1].
Tubulin/PARP1-IN-1 (20-40 nM; 24 h) reverses the epithelial-mesenchymal transition (EMT) phenotype of A549 cells[1].
Tubulin/PARP1-IN-1 (20-80 nM; 6 h) inhibits capillary-like tube formation in human umbilical vein endothelial cells (HUVECs) in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-29 cells
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Concentration:20, 40, 80 nM
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Incubation Time:24 h
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Result:Dose-dependently induced apoptosis in HT-29 cells, with the highest tested concentration increasing the apoptotic proportion to 25.4%.
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Cell Line:HT-29 cells
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Concentration:20, 40, 80 nM
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Incubation Time:24 h
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Result:Inducted of G2/M (M phase) blockade.
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Cell Line:A549 cells
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Concentration:20, 40 nM
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Incubation Time:24 h
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Result:Inhibited cell migration.
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Cell Line:A549 cells
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Concentration:20, 40 nM
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Incubation Time:24 h
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Result:Inhibited cell invasion,
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Cell Line:HT-29 and A549 cells
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Concentration:40, 80 nM
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Incubation Time:24 h
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Result:Increased Bax, Bim, Cleaved Caspase-3 and Cleaved PARP and dereased Bcl-2 in HT-29 cells.
Increased E-cadherin, decreased Vimentin and ZEB1 in A549 cells.
Parmacokinetics
| Species | Dose | Route | C0 | AUC0-t | AUC0-∞ | T1/2 | Vd/F | CL/F | MRT0-∞ |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 5 mg/kg | i.v. | 55763.18 ng/mL | 3080.51 ng·h/mL | 3085.78 ng·h/mL | 1.76 h | 4.16 L/kg | 1.63 L/h/kg | 0.47 h |
In Vivo
Tubulin/PARP1-IN-1 (10-20 mg/kg; i.v.; once every 3 days; administered for 14 days) potently inhibits hematogenous lung metastasis of colorectal cancer in BALB/c mice, reduces metastatic burden and alleviates pathological damage of lung tissue[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 nude mice (half male and half female, 4 weeks old)
[1] -
Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:i.v.; once every 3 days; administered for 28 days
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Result:Achieved a tumor inhibition rate of 76.55% at 20 mg/kg, with significant reductions in tumor volume and weight compared to controls.
Decreased expression of proliferation marker Ki67, reduced vascular endothelial marker CD31, and upregulated DNA damage marker γ-H2AX in tumor tissues.
Showed no significant body weight loss, no obvious pathological abnormalities in major organs (heart, liver, spleen, lung, kidney), and blood biochemical indicators (ALT, AST, CR, BUN, CK, LDH) remained within normal ranges.
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Animal Model:BALB/c mice (female, 4 weeks old)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:i.v.; once every 3 days; administered for 14 days
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Result:Significantly reduced the lung metastasis burden and the number of nodules, and inhibits hematogenous lung metastasis of colorectal cancer.
Chemical Information
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Molecular Weight 696.34
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Formula C30H24Br2N4O6
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SMILES
O=C(C1=C2C(N(C)C(CN3C(COC4=O)=C4[C@H](C5=CC(Br)=C(OC)C(Br)=C5)C6=C3C=C7C(OCCO7)=C6)=N2)=CC=C1)N
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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)
Tubulin/PARP1-IN-1 Related Classifications
HY-184277 Related Classifications
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