Tubulin-IN-51
Tubulin-IN-51 is an orally available, potent tubulin inhibitor (IC50 = 31 nM). Tubulin-IN-51 promotes tubulin polymerization in vitro and does not compete with Paclitaxel (HY-B0015) for binding. Tubulin-IN-51 inhibits the binding of Vinblastine (HY-13780) to tubulin. Tubulin-IN-51 downregulates the proportion of cells in the G1 phase and induces apoptosis. Tubulin-IN-51 inhibits tumor growth in multiple nude mouse xenograft models.
For research use only. We do not sell to patients.
- CAS No.: 849550-36-3
- Formula: C18H18ClF5N6O
- Molecular Weight:464.82
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Tubulin-IN-51 (Compound 8) promotes tubulin polymerization, a phenomenon similar to the effect of Paclitaxel (HY-B0015), preventes binding of [3H] Vinblastine (HY-13780) to tubulin[1].
Tubulin-IN-51 induces apoptosis by downregulating the proportion of cells in the G1 phase at low compound concentrations (10-35 nM) and arrests the G2/M phase at high compound concentrations (35-200 nM), a pattern similar to that observed with Paclitaxel (HY-B0015)[1].
Tubulin-IN-51 inhibits KB, KB 8.5, and KBV1 Cell Proliferation, with IC50s of 23 nM, 67 nM, 953 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Tubulin-IN-51 (Compound 8) (15-25 mg/kg, i.v., days 0, 7, 14, and 21 after staging) inhibits tumor growth in tumor (A549 human non-small cell lung carcinoma (NSCLC) cells) xenograft mice model[1].
Tubulin-IN-51 (2.5-50 mg/kg, p.o., days 0, 7 after staging) inhibits tumor growth in tumor (U87-MG human glioblastoma) xenograft mice model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Tumor (A549 human NSCLC cells) (i.p., 1x106) xenograft mice model[1]
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Dosage:15 mg/kg, 20 mg/kg, 25 mg/kg
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Administration:i.v. , on days 0, 7, 14, and 21 after tumor staging
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Result:Inhibited tumor growth.
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Animal Model:Tumor (U87-MG human glioblastoma) (i.p., 1x107) xenograft mice model[1]
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Dosage:2.5 mg/kg, 5 mg/kg, 10 mg/kg, 25 mg/kg, 50 mg/kg on day 0 only
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Administration:p.o., on days 0, 7 after tumor staging
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Result:Inhibited tumor growth.
Chemical Information
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CAS No. 849550-36-3
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Molecular Weight 464.82
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Formula C18H18ClF5N6O
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SMILES
FC1=CC(OCCCNC)=CC(F)=C1C2=C(N[C@@H](C(F)(F)F)C)N3N=CN=C3N=C2Cl
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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-IN-51 Related Classifications
HY-177021 Related Classifications
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