RN486
Based on 3 publication(s) in Google Scholar
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.
- Purity: 98.91%
- CAS No.: 1242156-23-5
- Formula: C35H35FN6O3
- Molecular Weight:606.69
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Immunology/Inflammation Compound Library
HY-L007
-
Kinase Inhibitor Library
HY-L009
-
Protein Tyrosine Kinase Compound Library
HY-L016
-
Orally Active Compound Library
HY-L061
-
Anti-Blood Cancer Compound Library
HY-L079
-
Autoimmune Disease Compound Library
HY-L156
-
Highly Selective Inhibitors Library
HY-L158
-
Serine/Threonine Kinase Inhibitor Library
HY-L164
-
Anti-Hematopathy Compound Library
HY-L171
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Protein Kinase Compound Library
HY-L196
-
High-Throughput Bioactive Compound Library
HY-L205
-
Anti-Rheumatic Arthritis Compound Library
HY-L210
-
Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) RN486
More
Customer Validation & Images
-
WB
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Macrophage | IC50 |
4 nM
Compound: 29, RN486
|
Inhibition of immobilized immune complex-stimulated TNFalpha production in macrophages
Inhibition of immobilized immune complex-stimulated TNFalpha production in macrophages
|
[PMID: 22394077] |
| Mast cell | IC50 |
29.2 nM
Compound: 29, RN486
|
Inhibition of IgE-Fce cross-linking induced histamine release in mast cells
Inhibition of IgE-Fce cross-linking induced histamine release in mast cells
|
[PMID: 22394077] |
| Ramos | IC50 |
27 nM
Compound: RN486
|
Inhibition of BTK in human Ramos cells assessed as reduction in IgM-induced calcium influx incubated for 20 mins by Fluo-4 dye based fluorescence assay
Inhibition of BTK in human Ramos cells assessed as reduction in IgM-induced calcium influx incubated for 20 mins by Fluo-4 dye based fluorescence assay
|
[PMID: 25515957] |
| Ramos | IC50 |
27.3 nM
Compound: 3, RN486
|
Inhibition of BTK in human Ramos cells after 20 mins by fluorescence assay
Inhibition of BTK in human Ramos cells after 20 mins by fluorescence assay
|
[PMID: 25596757] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1242156-23-5
-
Appearance Solid
-
Molecular Weight 606.69
-
Formula C35H35FN6O3
-
Color Off-white to light yellow
-
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 2 years -20°C 1 year
Publications (3)
-
Journal Impact Factor
-
Most Recent
-
Leukemia
BTK gatekeeper residue variation combined with cysteine 481 substitution causes super-resistance to irreversible inhibitors acalabrutinib, ibrutinib and zanubrutinib. [Abstract]2021 May;35(5):1317-1329. PMID: 33526860 -
Blood Adv
Novel mouse model resistant to irreversible BTK inhibitors: a tool identifying new therapeutic targets and side effects. [Abstract]2020 Jun 9;4(11):2439-2450. PMID: 32492159
RN486 purchased from MedChemExpress. Usage Cited in: Blood Adv. 2020 Jun 9;4(11):2439-2450. [Abstract]
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).
-
J Biomol Screen
2015 Aug;20(7):876-86. PMID: 25948491
Solvent & Solubility
DMSO : 24 mg/mL (39.56 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (272 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
[1]. Xu D, et al. RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents. J Pharmacol Exp Ther. 2012 Apr;341(1):90-103. [Content Brief]
[2]. Hsu J, et al. Bruton's Tyrosine Kinase mediates platelet receptor-induced generation of microparticles: a potential mechanism for amplification of inflammatory responses in rheumatoid arthritis synovial joints. Immunol Lett. 2013 Feb;150(1-2):97-104. [Content Brief]
[3]. Mina-Osorio P, et al. Suppression of glomerulonephritis in lupus-prone NZB × NZW mice by RN486, a selective inhibitor of Bruton's tyrosine kinase. Arthritis Rheum. 2013 Sep;65(9):2380-91. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6483 mL | 8.2414 mL | 16.4829 mL | 41.2072 mL |
| 5 mM | 0.3297 mL | 1.6483 mL | 3.2966 mL | 8.2414 mL | |
| 10 mM | 0.1648 mL | 0.8241 mL | 1.6483 mL | 4.1207 mL | |
| 15 mM | 0.1099 mL | 0.5494 mL | 1.0989 mL | 2.7471 mL | |
| 20 mM | 0.0824 mL | 0.4121 mL | 0.8241 mL | 2.0604 mL | |
| 25 mM | 0.0659 mL | 0.3297 mL | 0.6593 mL | 1.6483 mL | |
| 30 mM | 0.0549 mL | 0.2747 mL | 0.5494 mL | 1.3736 mL |
RN486 Related Classifications
HY-18018 Related Classifications
Powered by Bioz