2. Metabolic Enzyme/Protease Membrane Transporter/Ion Channel
  3. Cytochrome P450 P-glycoprotein
  4. 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.

CYP1B1-IN-14 TFA

CYP1B1-IN-14 TFA Chemical Structure

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CYP1B1-IN-14 TFA Related Antibodies

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

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Description

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[1].

IC50 & Target[1]

CYP1B1

1.32 nM (IC50)

CYP1B1

0.72 μM (Ki)

In Vitro

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.

CYP1B1-IN-14 TFA Related Antibodies

Cell Viability Assay[1]

Cell Line: Paclitaxel-resistant lung cancer cell lines (H460/PTX and A549/PTX)
Concentration: 5 μM (co-administered with PTX)
Incubation Time: 48 h
Result: Enhanced PTX's anticancer activity 26.5-fold in H460/PTX cells and 22.9-fold in A549/PTX cells, respectively.
In Vivo

CYP1B1-IN-14 (45 mg/kg; i.p.; once daily; 16 days) TFA alone does not inhibit the growth of A549/PTX xenografts, but exerts antitumor activity when combined with Paclitaxel (HY-B0015)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude treated A549/
PTX xenograft tumors (female, 4-6 weeks old)[1]
Dosage: 45 mg/kg
Administration: i.p.; once daily; 16 days
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.
Molecular Weight

641.27

Formula

C23H26Br2F3N3O5
SMILES

FC(F)(F)C(O)=O.CO/N=C(CC1=CC=CC=C1)/C(NCCC2=CC(Br)=C(C(Br)=C2)OCCCN)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CYP1B1-IN-14 TFA Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CYP1B1-IN-14Cytochrome P450P-glycoproteinCYPsP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243A549/PTX cellsxenograft modelspaclitaxel-resistant lung cancer17β-estradiolCHO-1B1 cellshCYP1B1H460/PTX cellspaclitaxelcancer cellsInhibitorinhibitorinhibit

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