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主营:抗癌化学试剂和激酶抑制剂
℡ 4000-520-616
℡ 4000-520-616
MedKoo/RN486featured/100mg/406103
产品编号:406103
市  场 价:¥23000.00
场      地:美国(厂家直采)
产品分类: 蛋白类>多肽>多肽合成>
联系QQ:1570468124
电话号码:4000-520-616
邮      箱: info@ebiomall.com
美  元  价:$1150.00
品      牌: MedKoo
公      司:MedKoo Biosciences, Inc
公司分类:
MedKoo/RN486featured/100mg/406103
商品介绍

RN486
featured

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

SizePriceShipping out timeQuantity
100mgUSD 11502 Weeks
200mgUSD 18502 Weeks
500mgUSD 32502 Weeks
1gUSD 46502 Weeks
2gUSD 64502 Weeks
5gUSD 89502 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-01-23.Prices are subject to change without notice.

RN486, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received.

Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 406103Name: RN486CAS#: 1242156-23-5Chemical Formula: C35H35FN6O3Exact Mass: 606.27547Molecular Weight: 606.69Elemental 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).

HS Tariff Code:
2934.99.9001

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, MinS, 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 inhibitorof 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-baseddrug 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 MedChem. 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 Kinasemediates 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. EurJ 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.

品牌介绍
MedKoo,由化学家和药学家陈清奇博士。北卡罗莱纳州的研究三角区(Research Triangle Park, 简称 RTP ),是一家以研发、生产和销售小分子抗癌化合物为主的医药科技公司,该公司的业务范围主要是为全球所有从事抗癌药物研究和开发的制药公司,高校,研究院所,政府相关机构提供与抗癌药物分子相关的产品、试剂和技术服务。
中文名MedKoo中    文美帝药库医药科技公司创立于2008年总部位于美国东海岸
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