TACC3 inhibitor 2
TACC3 inhibitor 2 is a TACC3 inhibitor with improved metabolic stability, bioavailability, and strong potency.TACC3 inhibitor 2 binds to TACC3 to modulate its function. TACC3 inhibitor 2 induces mitotic arrest, apoptosis, and DNA damage. TACC3 inhibitor 2 can be used for the research of breast cancer, colon cancer.
For research use only. We do not sell to patients.
- CAS No.: 2642351-96-8
- Formula: C20H22FN5O2
- Molecular Weight:383.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
TACC3 inhibitor 2 (Compound 13b) potently inhibits the proliferation of JIMT-1 breast cancer cells with high TACC3 expression, with an IC50 of 0.2 μM[1].
TACC3 inhibitor 2 (10 μM) specifically binds to TACC3 in MDA-MB-231 and MDA-MB-157 triple-negative breast cancer cells, and protects this protein from pronase digestion at a concentration of 10 μM[1].
TACC3 inhibitor 2 preferentially inhibits the proliferation of MDA-MB-157, HCT-116 and RKO cancer cells with high TACC3 expression, with IC50 values of 0.86 μM, 0.31 μM and 0.20 μM, respectively, while shows weak activity against MCF-7 cells and HT-29 colon cancer cells with low TACC3 expression[1].
TACC3 inhibitor 2 (0.05-0.5 μM; 12-14 d) reduces the colony-forming ability of MDA-MB-157, HCC38, MDA-MB-231, BT-20 and CT-26 cancer cells in a dose-dependent manner under the treatment condition of 0.05-0.5 μM for 12-14 days[1].
TACC3 inhibitor 2 (200 nM) induces mitotic arrest, apoptosis and DNA damage in JIMT-1 breast cancer cells, and increases the levels of p-Histone H3 (Ser10), cleaved PARP and p-H2AX (Ser139)[1].
The metabolic stability of TACC3 inhibitor 2 in human liver microsomes is significantly improved, with a half-life of 78.72 min and an intrinsic clearance rate of 17.7 μL/min/mg[1].
TACC3 inhibitor 2 shows no significant inhibitory effect on CYP1A2, 2A6, 2B6, 2D6 and 2E1, weak inhibitory effect on CYP2C8, CYP2C9, CYP3A4-M and CYP3A4-T, and moderate inhibitory effect on CYP2C19 (IC50=2.17 μM)[1].
TACC3 inhibitor 2 exhibits favorable hERG safety profiles, with an IC50 of 17.16 μM for its inhibitory effect on hERG channels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human MDA-MB-157, HCC38, MDA-MB-231, BT-20 breast cancer cells, and mouse CT-26 colon cancer cells
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Concentration:0.05-0.2 μM (breast cancer cells); 0.1-0.5 μM (CT-26 cells)
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Incubation Time:14 days (breast cancer cells); 12 days (CT-26 cells)
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Result:Significantly reduced the number of viable colonies in all tested cancer cell lines in a dose-dependent manner.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD1 mice[1]
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Dosage:10 mg/kg (i.v.); 50 mg/kg (p.o.)
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Administration:i.v.; single dose; p.o.; single dose
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Result:Exhibited a terminal half-life of 1.76 h, volume of distribution of 2.78 L/kg, initial plasma concentration (C0) of 6370 ng/mL, clearance of 31.6 mL/min/kg, and AUC of 5356 h*ng/mL after i.v. administration.
Exhibited a terminal half-life of 2.36 h, Cmax of 1453 ng/mL, AUC of 17179 h*ng/mL, and oral bioavailability of 62.9% after oral administration with formulation A.
Exhibited a terminal half-life of 2.06 h, Cmax of 1710 ng/mL, AUC of 21550 h*ng/mL, and oral bioavailability of 79.7% after oral administration with formulation B.
Chemical Information
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CAS No. 2642351-96-8
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Molecular Weight 383.42
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Formula C20H22FN5O2
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SMILES
CC1CCN(C2=NC=CC(NC3=CC(C4=CC=C(OC)C=C4F)=NO3)=N2)CC1
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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)