IDO/Tubulin-IN-2
IDO/Tubulin-IN-2 (HT2) is a potent TDO and tubulin inhibitor. IDO/Tubulin-IN-2 also shows potent activity against U87, HepG2, A549, HCT-116, and LO2 cancer cell lines, with IC50 values of 0.43, 0.036, 0.041, 0.095 and 1.04 μM, respectively. IDO/Tubulin-IN-2 remarkably promotes the antitumor activity.
For research use only. We do not sell to patients.
- CAS No.: 2409479-24-7
- Formula: C48H40N6O10
- Molecular Weight:860.87
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
TDO, Tubulin[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.041 μM
Compound: HT2
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Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
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[PMID: 31830637] |
| HCT-116 | IC50 |
0.095 μM
Compound: HT2
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Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
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[PMID: 31830637] |
| HepG2 | IC50 |
0.036 μM
Compound: HT2
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Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
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[PMID: 31830637] |
| L02 | IC50 |
1.04 μM
Compound: HT2
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Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
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[PMID: 31830637] |
| U-87MG ATCC | IC50 |
0.43 μM
Compound: HT2
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Antiproliferative activity against human U87 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human U87 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
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[PMID: 31830637] |
IDO/Tubulin-IN-2 (HT2) (0-50 μM, 4 h) shows potent cytotoxicity with IC50 values between 0.036 and 0.43 μM against cancer cell lines[1].
IDO/Tubulin-IN-2 (0.1 μM, 24 h) arrests the HepG2 cells cycle mainly at the G2 phase[1].
IDO/Tubulin-IN-2 (0.1 μM, 24 h) can effectively cause cell apoptosis[1].
IDO/Tubulin-IN-2 (0.1 μM, 24 h) has strongly effects on inducing the proteolytic cleavage of PARP and up-regulating the expression level of caspase-3[1].
IDO/Tubulin-IN-2 (0.05 μM, 24, 48 and 72 h) markedly decreases mRNA expression level of TDO at a time-dependent manner[1].
IDO/Tubulin-IN-2 (2 days) can improve T-cell activation and proliferation and enhance immune response[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human cancer cell lines and non-tumoral cell line[1]
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Concentration:0-50 μM
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Incubation Time:4 h
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Result:Displayed potent cytotoxicity with IC50 values of 0.43 μM (U87), 0.036 μM (HepG2), 0.041 μM (A549), 0.095 μM (HCT-116), and 1.04 μM (LO2).
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Cell Line:HepG2 cells[1]
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Concentration:0.1 μM
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Incubation Time:24 h
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Result:Arrested the HepG2 cells cycle mainly at the G2 phase.
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Cell Line:HepG2 cells[1]
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Concentration:0.1 μM
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Incubation Time:24 h
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Result:Effectively caused cell apoptosis, the percentage of apoptosis cells increased to 54%
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Cell Line:HepG2 cells[1]
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Concentration:0.1 μM
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Incubation Time:24 h
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Result:Showed strongly effects on inducing the proteolytic cleavage of PARP and up-regulating the expression level of caspase-3, which could lead to cell death at last.
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Cell Line:HepG2 cells[1]
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Concentration:0.05 μM
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Incubation Time:24, 48 and 72 h
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Result:Markedly decreased mRNA expression level of TDO at a time-dependent manner.
IDO/Tubulin-IN-2 (30 mg/kg; IV; 29 days) has effective antitumor immunity ability to promote the tumor therapeutic efficacy[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (mouse liver cancer xenograft models, established by subcutaneous inoculation of H22 cells)[1]
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Dosage:30 mg/kg
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Administration:Intravenously injected via a tail vein; daily, for 21 days
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Result:Significantly inhibited tumor growth.
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Animal Model:Male A549 tumor xenograft BALB/c nude mice (5 weeks, 18-22 g)[1]
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Dosage:30 mg/kg
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Administration:IV, daily, for 29 days
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Result:Had effective antitumor immunity ability to promote the tumor therapeutic efficacy.
Chemical Information
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CAS No. 2409479-24-7
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Molecular Weight 860.87
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Formula C48H40N6O10
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SMILES
COC1=CC=C(C=C1OC(C2=CC=CC(CN3C=C(N=N3)CCOC(C4=CC=CC(CN5N=NC6=C5C(C7=CC=CC=C7C6=O)=O)=C4)=O)=C2)=O)/C=C\C8=CC(OC)=C(C(OC)=C8)OC
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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)
IDO/Tubulin-IN-2 Related Classifications
HY-146715 Related Classifications
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