IG-105
IG-105 is a potent tubulin inhibitor, with an IC50 of 0.6 μM for competitive inhibition of [3H] colchicine binding to tubulin, and an IC50 of 3 μM for inhibition of tubulin polymerization. IG-105 inhibits microtubule polymerization by binding to the colchicine pocket of tubulin, induces cell cycle arrest at the G2-M phase, and subsequently activates the caspase cascade through Bcl-2 inactivation and p53 upregulation to induce apoptosis. As a non-Pgp substrate, IG-105 effectively overcomes multidrug resistance. IG-105 can be used in the research of leukemia, breast cancer, liver cancer, prostate cancer, lung cancer, melanoma, pancreatic cancer and colon cancer.
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- CAS No.: 905978-63-4
- Formule: C20H19N3O4S
- Masse moléculaire:397.45
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LoVo | IC50 |
0.298 μM
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Antiproliferative activity against human LoVo colon cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Antiproliferative activity against human LoVo colon cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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18829501 |
| NCI-H23 | IC50 |
0.274 μM
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Antiproliferative activity against human NCI-H23 lung cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Antiproliferative activity against human NCI-H23 lung cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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18829501 |
| HUVEC | IC50 |
2.52 μM
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Antiproliferative activity against non-malignant human HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Antiproliferative activity against non-malignant human HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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18829501 |
| SMMC-7721 | IC50 |
0.528 μM
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Antiproliferative activity against drug-resistant human SMMC-7721 hepatoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Antiproliferative activity against drug-resistant human SMMC-7721 hepatoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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18829501 |
| Bel-7402 | IC50 |
0.179 μM
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Antiproliferative activity against naive human Bel-7402 hepatoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Antiproliferative activity against naive human Bel-7402 hepatoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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18829501 |
| MCF7-DOX | IC50 |
0.199 μM
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Antiproliferative activity against Pgp-overexpressing drug-resistant human MCF-7/Dox/Pgp breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Antiproliferative activity against Pgp-overexpressing drug-resistant human MCF-7/Dox/Pgp breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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18829501 |
| MCF7 | IC50 |
0.151 μM
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Antiproliferative activity against naive human MCF-7 breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Antiproliferative activity against naive human MCF-7 breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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18829501 |
IG-105 (up to 1 μM; 72 h) exerts significant inhibitory effects on cell growth and viability in CEM, Molt-3, DND-1, MIA PaCa-2, MCF-7, Bel-7402, SW620, LoVo, DU-145, NCI-H23, SMMC-7721, MCF-7/Dox/Pgp and HUVEC cells, with IC50 values ranging from 0.012 to 0.298 μM; in contrast, its inhibitory activity against non-malignant HUVEC cells is much weaker (IC50 = 2.52 μM)[1].
IG-105 (2 μM) does not stimulate P-glycoprotein (Pgp) ATPase activity in a cell-free system[1].
IG-105 (0.16-6 μM; 30 min) potently inhibits tubulin polymerization in a cell-free system with an IC50 of 3 μM. It also competitively inhibits [3H]colchicine binding with an IC50 of 0.6 μM, and does not interact with the vinca alkaloid binding pocket[1].
IG-105 (0.35 μM; 12 h) disrupts the cellular microtubule network and induces microtubule depolymerization in human hepatocellular carcinoma Bel-7402 cells[1].
IG-105 (0.35 μM; 3-36 h) induces G2-M phase arrest in human hepatocellular carcinoma cell line Bel-7402, upregulates cyclin B1 protein expression and downregulates cyclin D1 protein expression in a time-dependent manner, induces Bcl-2 phosphorylation, promotes caspase-3 cleavage, and upregulates the expressions of p53 and p21[1].
IG-105 (0.086-0.346 μM for 48 h and 0.35 μM for 12-48 h) induces apoptotic DNA fragmentation in human hepatocellular carcinoma Bel-7402 cells[1].
IG-105 (0.35 μM; 6-24 h) significantly enhances the activities of caspase-9, caspase-8, and caspase-3 in human hepatocellular carcinoma Bel-7402 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Bel-7402
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Concentration:0.35 μM
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Incubation Time:3, 6, 9, 12, 18, 24 h
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Result:Induced a significant accumulation and arrest of cells in the G2-M phase, accompanied by a decrease in the number of cells in the G0-G1 phase.
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Cell Line:Bel-7402
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Concentration:0.35 μM
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Incubation Time:3, 6, 9, 12, 18, 24, 36 h
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Result:Led to a time-dependent up-regulation of mitotic cyclin B1 protein expression and a decrease in G0-G1 phase cyclin D1 protein expression.
Induced phosphorylation of Bcl-2 protein and cleavage activation of caspase-3, and caused time-dependent up-regulation of p53 and p21 protein expression.
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Cell Line:Bel-7402
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Concentration:0.35 μM
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Incubation Time:12 h
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Result:Caused the disruption of the intracellular microtubule network, showing short and curled microtubule fragments, and resulted in reduced microtubule density.
IG-105 (100-200 mg/kg; i.p.; once every two days; starting on day 14 after tumor inoculation) significantly inhibits tumor growth in a subcutaneous xenograft model of human breast cancer[1].
IG-105 (175 mg/kg; i.p.; once every two days; starting on day 11 post tumor implantation) converts subcurative doses of drugs into a synergistic complete control of tumor growth when combined with Oxaliplatin (HY-17371) or Doxorubicin (HY-15142) in a human hepatocellular carcinoma subcutaneous xenograft model[1].
IG-105 (400-1000 mg/kg; i.p.; single administration; observation for 15 days) exhibits favorable safety in the acute toxicity model of healthy mice, with no lethal or significant pathological toxicity observed[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Kunming mice (female, 18-20 g)[1]
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Dosage:400 mg/kg; 550 mg/kg; 700 mg/kg; 850 mg/kg; 1000 mg/kg
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Administration:i.p.; single dose; for 15 days
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Result:Caused no death or body weight loss even at the extremely high dose of 1000 mg/kg.
Histopathologic examination (H&E staining) revealed no evidence of pathologic damage in major organs such as liver, kidney, heart, lung, and spleen.
Chemical Information
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CAS No. 905978-63-4
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Masse moléculaire 397.45
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Formule C20H19N3O4S
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SMILES
O=S(C1=CC2=C(C=C1)N(C)C3=C2C=CC=C3)(NC4=CC=C(OC)N=C4OC)=O
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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)
IG-105 Related Classifications
HY-111175 Related Classifications
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