RN486
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406103

CAS#: 1242156-23-5

Description: RN486 is a Bruton's tyrosine kinase (Btk) inhibitor. RN486 not only potently and selectively inhibited the Btk enzyme, but also displayed functional activities in human cell-based assays in multiple cell types, blocking Fcε receptor cross-linking-induced degranulation in mast cells (IC(50) = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC(50) = 7.0 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC(50) = 21.0 nM).


Price and Availability

Size
Price

10mg
USD 150
100mg
USD 750
1g
USD 3850
Size
Price

25mg
USD 250
200mg
USD 1350
2g
USD 5950
Size
Price

50mg
USD 450
500mg
USD 2650
5g
USD 8250

RN486, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 406103
Name: RN486
CAS#: 1242156-23-5
Chemical Formula: C35H35FN6O3
Exact Mass: 606.27547
Molecular Weight: 606.69
Elemental Analysis: C, 69.29; H, 5.81; F, 3.13; N, 13.85; O, 7.91


Synonym: RN486; RN-486; RN 486

IUPAC/Chemical Name: 6-cyclopropyl-8-fluoro-2-(2-hydroxymethyl-3-{1-methyl-5-[5-(4-methyl-piperazin-1-yl)-pyridin-2-ylamino]-6-oxo-1,6-dihydro-pyridin-3-yl}-phenyl)-2H-isoquinolin-1-one

InChi Key: ZTUJNJAKTLHBEX-UHFFFAOYSA-N

InChi Code: InChI=1S/C35H35FN6O3/c1-39-12-14-41(15-13-39)26-8-9-32(37-19-26)38-30-18-25(20-40(2)34(30)44)27-4-3-5-31(28(27)21-43)42-11-10-23-16-24(22-6-7-22)17-29(36)33(23)35(42)45/h3-5,8-11,16-20,22,43H,6-7,12-15,21H2,1-2H3,(H,37,38)

SMILES Code: O=C1N(C2=CC=CC(C(C=C3NC4=NC=C(N5CCN(C)CC5)C=C4)=CN(C)C3=O)=C2CO)C=CC6=C1C(F)=CC(C7CC7)=C6


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

  
 
 
 


References

1: Mina-Osorio P, LaStant J, Keirstead N, Whittard T, Ayala J, Stefanova S, Garrido R, Dimaano N, Hilton H, Giron M, Lau KY, Hang J, Postelnek J, Kim Y, Min S, Patel A, Woods J, Ramanujam M, DeMartino J, Narula S, Xu D. 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. doi: 10.1002/art.38047. PubMed PMID: 23754328.

2: Xu D, Kim Y, Postelnek J, Vu MD, Hu DQ, Liao C, Bradshaw M, Hsu J, Zhang J, Pashine A, Srinivasan D, Woods J, Levin A, O'Mahony A, Owens TD, Lou Y, Hill RJ, Narula S, DeMartino J, Fine JS. 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. doi: 10.1124/jpet.111.187740. PubMed PMID: 22228807.

3: Lou Y, Han X, Kuglstatter A, Kondru RK, Sweeney ZK, Soth M, McIntosh J, Litman R, Suh J, Kocer B, Davis D, Park J, Frauchiger S, Dewdney N, Zecic H, Taygerly JP, Sarma K, Hong J, Hill RJ, Gabriel T, Goldstein DM, Owens TD. Structure-based drug design of RN486, a potent and selective Bruton's tyrosine kinase (BTK) inhibitor, for the treatment of rheumatoid arthritis. J Med Chem. 2015 Jan 8;58(1):512-6. doi: 10.1021/jm500305p. PubMed PMID: 24712864.

4: Hartkamp LM, Fine JS, van Es IE, Tang MW, Smith M, Woods J, Narula S, DeMartino J, Tak PP, Reedquist KA. Btk inhibition suppresses agonist-induced human macrophage activation and inflammatory gene expression in RA synovial tissue explants. Ann Rheum Dis. 2015 Aug;74(8):1603-11. doi: 10.1136/annrheumdis-2013-204143. PubMed PMID: 24764451.

5: Zhao X, Huang W, Wang Y, Xin M, Jin Q, Cai J, Tang F, Zhao Y, Xiang H. Discovery of novel Bruton's tyrosine kinase (BTK) inhibitors bearing a pyrrolo[2,3-d]pyrimidine scaffold. Bioorg Med Chem. 2015 Feb 15;23(4):891-901. doi: 10.1016/j.bmc.2014.10.043. PubMed PMID: 25596757.

6: Zhao X, Xin M, Huang W, Ren Y, Jin Q, Tang F, Jiang H, Wang Y, Yang J, Mo S, Xiang H. Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors. Bioorg Med Chem. 2015 Jan 15;23(2):348-64. doi: 10.1016/j.bmc.2014.11.006. PubMed PMID: 25515957.

7: Hsu J, Gu Y, Tan SL, Narula S, DeMartino JA, Liao C. 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. doi: 10.1016/j.imlet.2012.12.007. PubMed PMID: 23266841.

8: Wang J, Lau KY, Jung J, Ravindran P, Barrat FJ. Bruton's tyrosine kinase regulates TLR9 but not TLR7 signaling in human plasmacytoid dendritic cells. Eur J Immunol. 2014 Apr;44(4):1130-6. doi: 10.1002/eji.201344030. PubMed PMID: 24375473.

9: Zhao X, Huang W, Wang Y, Xin M, Jin Q, Cai J, Tang F, Zhao Y, Xiang H. Pyrrolo[2,3-b]pyridine derivatives as potent Bruton's tyrosine kinase inhibitors. Bioorg Med Chem. 2015 Aug 1;23(15):4344-53. doi: 10.1016/j.bmc.2015.06.023. PubMed PMID: 26169764.