CYP1B1-IN-14 TFA
CYP1B1-IN-14 TFA is a metabolically stable hCYP1B1 competitive inhibitor with an IC50 of 1.32 nM and a Ki of 0.72 μM. CYP1B1-IN-14 TFA reverses the resistance of cancer cells to Paclitaxel (HY-B0015). CYP1B1-IN-14 TFA acts synergistically with Paclitaxel (HY-B0015) to inhibit tumor growth in xenograft models without obvious toxicity. CYP1B1-IN-14 TFA can be used for the research of cancers such as paclitaxel-resistant lung cancer.
For research use only. We do not sell to patients.
- Formula: C23H26Br2F3N3O5
- Molecular Weight:641.27
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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
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CYP1B1 1.32 nM (IC50) |
CYP1B1 0.72 μM (Ki) |
CYP1B1-IN-14 (compound 26a) (0-32 μM; 8 h) TFA inhibits cellular hCYP1B1 activity in CHO-1B1 cells with an IC50 of 2.21 μM[1].
CYP1B1-IN-14 (5 μM; 48 h) TFA reverses Paclitaxel (HY-B0015) resistance in H460/PTX and A549/PTX cells[1].
CYP1B1-IN-14 (1-10 μM; 2.75 h) TFA dose-dependently inhibits the function of P-gp transporter in MDR1-MDCK cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Paclitaxel-resistant lung cancer cell lines (H460/PTX and A549/PTX)
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Concentration:5 μM (co-administered with PTX)
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Incubation Time:48 h
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Result:Enhanced PTX's anticancer activity 26.5-fold in H460/PTX cells and 22.9-fold in A549/PTX cells, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude treated A549/
PTX xenograft tumors (female, 4-6 weeks old)[1] -
Dosage:45 mg/kg
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Administration:i.p.; once daily; 16 days
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Result:Showed no influence on tumor growth when administered alone.
Produced a synergistic antitumor effect with a 41.1% tumor growth inhibition rate when co-administered with Paclitaxel.
Caused no animal death or notable body weight loss.
Chemical Information
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Molecular Weight 641.27
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Formula C23H26Br2F3N3O5
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SMILES
FC(F)(F)C(O)=O.CO/N=C(CC1=CC=CC=C1)/C(NCCC2=CC(Br)=C(C(Br)=C2)OCCCN)=O
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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)
CYP1B1-IN-14 TFA Related Classifications
HY-181550A Related Classifications
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