Tubulin polymerization-IN-81
Tubulin polymerization-IN-81 is a selective Tubulin inhibitor with an IC50 of 5.41 μM. Tubulin polymerization-IN-81 possesses a significant anti-proliferative activity, unique ROS-mediated apoptotic mechanism and potent anti-microtubule activity. Tubulin polymerization-IN-81 can be used in anti-tumor research.
For research use only. We do not sell to patients.
- Formula: C27H23N5O5
- Molecular Weight:497.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
Tubulin polymerization-IN-81 (Compound 4a) (10 μM) exhibits potent activity against fifteen cancer cell lines and is lethal to SF-539 and CAKI-1 with GI = 112.22 % and 150.64 %, respectively[1].
Tubulin polymerization-IN-81 can inhibit the proliferation of various cell lines[1].
Tubulin polymerization-IN-81 (6 μM, 20 min) has a tubulin inhibition activity with an IC50 of 5.41 μM, hindering microtubule polymerization in A549 cells[1].
Tubulin polymerization-IN-81 (5.93 μM, 48 h) prevents cancer cell proliferation by arresting the cell cycle at the G2/M phase in A549 cells (34.8%) [1].
Tubulin polymerization-IN-81 (5.93 μM, 48 h) displays significantly high levels of ROS generation and exhibits a 2.4 fold increase in A549 cells[1].
Tubulin polymerization-IN-81 (5.93 μM, 48 h) induces 85% cell death of the total cells, mainly in the early stage in A549 cells[1].
Tubulin polymerization-IN-81 (5.93 μM, 48 h) displays significant loss of MMP by approximately 56- 67 % in A549 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OVCAR-4, A549, WI-38
leukemia (MOLT-4 and RPMI-8226), colon cancer (HCT-15), melanoma (LOX IMIV), renal cancer (CAKI-1), ovarian cancer (NCI/ADR-RES) and breast cancer (BT-549 and MDA-MB-468)
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Concentration:10 μM
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Incubation Time:48 h
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Result:Exhibited potent activity against fifteen cancer cell lines, including (A549/ATCC, HOP-92, NCI-H226, SF-268, SNB-19, SNB-75, U251, SK-MEL-28, UACC-257, OVCAR-3, OVCAR-4, OVCAR-8, HS 578T) with growth inhibition range of 60.88%-86.51%.
Exhibited mean inhibition against all nine cancer cell lines of 41.03%.
Showed the highest anti-proliferative activity against both cell lines with IC50 = 3.46 and 5.93 μM against OVCAR-4 and A549, respectively.
Showed weak activity towards non-tumor cells WI-38 with IC50 value 42.71 μM.
Demonstrated better safety towards WI-38 cells (IC50 = 42.71 μM) than CA-4, with a selectivity index (SI*) equal to 7.20.
Chemical Information
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Molecular Weight 497.50
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Formula C27H23N5O5
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SMILES
O=CN1N=C(C2=CC=CC=C2)CC1C3=CN(C4=CC=C([N+]([O-])=O)C=C4)N=C3C5=CC=C(OC)C(OC)=C5
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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)