2. Protein Tyrosine Kinase/RTK
    Membrane Transporter/Ion Channel
  3. Btk
    BCRP
  4. PCI 29732

PCI 29732 

Cat. No.: HY-18010 Purity: 99.86%
COA Handling Instructions

PCI 29732 is a potent, orally active, reversible BTK inhibitor with Kiapp values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2.

For research use only. We do not sell to patients.

PCI 29732 Chemical Structure

PCI 29732 Chemical Structure

CAS No. : 330786-25-9

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Solution
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
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10 mM * 1 mL
ready for reconstitution
 USD 110 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
50 mg USD 560 In-stock
Estimated Time of Arrival: December 31
100 mg USD 980 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    PCI 29732 purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;48(6):2302-2317.  [Abstract]

    Effects of PCI29732 on total and phosphorylated levels of AKT and ERK1/2. S1-MI-80 cells are treated with various concentrations (0-3 μM) of PCI29732 for 48 h, or with 1.5 μM of PCI29732 for 24, 48, or 72 h.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PCI 29732 is a potent, orally active, reversible BTK inhibitor with Kiapp values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2[1][2].

    In Vitro

    PCI29732 shows cytotoxicity in different cells. The IC50 values are 7.94 μM for S1, 7.79 μM for S1-MI-80, 6.55 μM for H460, 6.34 μM for H460/MX20, 6.14 μM for KB, 6.02 μM for KBv200, 12.45 μM for HEK293/pcDNA3, 14.58 μM for HEK293-ABCG2-482-R2, and 13.24 μM for HEK293-ABCG2-482-T7 cells[2].
    PCI-29732 blocks the transcriptional up-regulation of a panel of B-cell activation genes in human CD20+ B cells stimulated at the B-cell antigen receptor (BCR)[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    In Vivo

    PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 and enhances the anti-tumor efficacy of substrate chemotherapeutic agents[2].
    PCI 29732 (20 mg/kg; p.o.; every 3 d × 5 times) enhances the anticancer efficacy of Topotecan in the H460/MX20 cell xenograft nude mice model[2].

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

    Animal Model: 5-6 weeks old athymic nude mice (bearing H460/MX20 cells)[2]
    Dosage: 20 mg/kg (combination with Topotecan; every 3 d × 5 times, i.p., 3 mg/kg; topotecan was given 1 h after PCI29732 administration)
    Administration: P.o.; every 3 d × 5 times
    Result: Significant reductions in tumor weight and volume were observed in the group treated with PCI29732 in combination with Topotecan.
    Molecular Weight

    371.44

    Appearance

    Solid

    Formula

    C22H21N5O
    CAS No.
    SMILES

    NC1=NC=NC2=C1C(C3=CC=C(OC4=CC=CC=C4)C=C3)=NN2C5CCCC5
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 53 mg/mL (142.69 mM)

    Ethanol : 10 mg/mL (26.92 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6922 mL 13.4611 mL 26.9222 mL
    5 mM 0.5384 mL 2.6922 mL 5.3844 mL
    10 mM 0.2692 mL 1.3461 mL 2.6922 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 1 mg/mL (2.69 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% EtOH    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 1 mg/mL (2.69 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% EtOH    90% corn oil

      Solubility: ≥ 1 mg/mL (2.69 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation
    References
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    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.

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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

    Keywords:

    PCI 29732330786-25-9PCI29732PCI-29732BtkBCRPBruton tyrosine kinaseBreast cancer resistance proteinABCG2cytotoxicityBCRreversibleoralB-cellInhibitorinhibitorinhibit

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