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Poseltinib
CAS No. 1353552-97-2
Poseltinib( HM-71224 | LY-3337641 )
Catalog No. M11439 CAS No. 1353552-97-2
Poseltinib (HM-71224, LY-3337641) is a potent and selective, covalent inhibitor of Btk with IC50 of 1.95 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
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| 10MG | 314 | In Stock |
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| 50MG | 784 | In Stock |
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Biological Information
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Product NamePoseltinib
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NoteResearch use only, not for human use.
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Brief DescriptionPoseltinib (HM-71224, LY-3337641) is a potent and selective, covalent inhibitor of Btk with IC50 of 1.95 nM.
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DescriptionPoseltinib (HM-71224, LY-3337641) is a potent and selective, covalent inhibitor of Btk with IC50 of 1.95 nM; also inhibits BMX, TEC, TXK, EGFR in biochemical sense (IC50=0.3-2.5 nM); effectively inhibits the phosphorylation of Btk and PLCγ2, and inhibits expression of CD40, CD69, and CD86 by activated primary human B cells with IC50 of 4.2, 4.2, and 7.7 nM, respectively; inhibited the production of TNF-α, IL-6, and IL-1β by human monocytes, and osteoclast formation by human monocytes; ameliorates arthritis in a mouse model.Rheumatoid Arthritis Phase 1 Clinical.
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In VitroWestern Blot Analysis Cell Line: B cells Concentration:0.1-100 nM Incubation Time:30 min Result:Blocked both autophosphorylation of BTK and phosphorylation of PLCγ2 with IC50 values of less than 10 nM.Decreased the production of both TNF-α and IL-6 in a dose-dependent manner.
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In VivoAnimal Model:MRL/lpr mice and NZB/W F1 mice modelsDosage:3-30 mg/kg Administration:p.o Result:Decreased the spleen weights and prevented skin lesion progression.Ameliorated renal injury and inflammation and improved the survival rate.Animal Model:Collagen-induced arthritis (CIA) mouse model Dosage:1-30 mg/kg Administration:p.o Result:Reduced the serum IL-6, circulating anti-collagen antibodies and total IgG levels.Reduced erosive bone changes and prevented bone loss.
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SynonymsHM-71224 | LY-3337641
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PathwayTyrosine Kinase
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TargetBTK
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RecptorBTK
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Research AreaInflammation/Immunology
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IndicationRheumatoid Arthritis
Chemical Information
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CAS Number1353552-97-2
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Formula Weight470.533
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Molecular FormulaC26H26N6O3
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 100 mg/mL (212.53 mM)
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SMILESC=CC(NC1=CC=CC(OC2=C(OC=C3)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1)=O
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Chemical Name2-Propenamide, N-[3-[[2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]furo[3,2-d]pyrimidin-4-yl]oxy]phenyl]-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Park JK, et al. Arthritis Res Ther. 2016 Apr 18;18:91.
2. Akinleye A, et al. J Hematol Oncol. 2013 Aug 19;6:59.
3. Smith PF, et al. Br J Clin Pharmacol. 2017 Jun 21.
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