1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. RN486

RN486 

Cat. No.: HY-18018 Purity: 99.87%
Handling Instructions

RN486 is a potent, selective and orally active Btk inhibitor with an IC50 of 4.0 nM and a Kd of 0.31 nM. RN486 is less active for other kinases. RN486 can be used for rheumatoid arthritis and systemic lupus erythematosus research.

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

RN486 Chemical Structure

RN486 Chemical Structure

CAS No. : 1242156-23-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 208 In-stock
Estimated Time of Arrival: December 31
1 mg USD 96 In-stock
Estimated Time of Arrival: December 31
5 mg USD 156 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
25 mg USD 432 In-stock
Estimated Time of Arrival: December 31
50 mg USD 660 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    RN486 purchased from MCE. Usage Cited in: Blood Adv. 2020 Jun 9;4(11):2439-2450.

    Western blot on whole-cell lysates from B cells with indicated genotype (wild-type or C481S), inhibitor treatment (ibrutinib or RN486) and stimulation (anti-IgM and H2O2).
    • Biological Activity

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    • References

    • Customer Review

    Description

    RN486 is a potent, selective and orally active Btk inhibitor with an IC50 of 4.0 nM and a Kd of 0.31 nM. RN486 is less active for other kinases. RN486 can be used for rheumatoid arthritis and systemic lupus erythematosus research[1][2][3].

    IC50 & Target

    IC50: 4.0 nM (Btk)[1]
    Kd: 0.31 nM (Btk)[1]

    In Vitro

    RN486 blocks Fcε receptor cross-linking-induced degranulation in mast cells (IC50 = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC50 = 7 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC50 = 21 nM)[1].
    In a co-culture system consisting of human primary synovial FLS and activated human platelets, convulxin stimulation resulted in elevated production of pro-inflammatory cytokines, IL-6 and IL-8, an effect which is dose-dependently blocked by RN486[2].

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

    In Vivo

    RN486 produces robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 (1-30 mg/kg) inhibits both joint and systemic inflammation, reducing both paw swelling and inflammatory markers in the blood[1].

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

    Molecular Weight

    606.69

    Formula

    C₃₅H₃₅FN₆O₃

    CAS No.

    1242156-23-5

    SMILES

    O=C1C(NC2=CC=C(N3CCN(C)CC3)C=N2)=CC(C4=CC=CC(N5C=CC(C=C(C6CC6)C=C7F)=C7C5=O)=C4CO)=CN1C

    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 : 24 mg/mL (39.56 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6483 mL 8.2414 mL 16.4829 mL
    5 mM 0.3297 mL 1.6483 mL 3.2966 mL
    10 mM 0.1648 mL 0.8241 mL 1.6483 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References

    Purity: 99.87%

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    Keywords:

    RN486RN 486RN-486BtkBruton tyrosine kinaseInhibitorinhibitorinhibit

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    Product Name:
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    Cat. No.:
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