Poseltinib
- Product Name
- Poseltinib
- CAS No.
- 1353552-97-2
- Chemical Name
- Poseltinib
- Synonyms
- LY-3337641);Poseltinib (HM-71224;Poseltinib (HM71224, LY3337641);2-Propenamide, N-[3-[[2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]furo[3,2-d]pyrimidin-4-yl]oxy]phenyl]-
- CBNumber
- CB74204131
- Molecular Formula
- C26H26N6O3
- Formula Weight
- 470.52
- MOL File
- 1353552-97-2.mol
Poseltinib Property
- Density
- 1.316±0.06 g/cm3(Predicted)
- solubility
- DMSO:100.0(Max Conc. mg/mL);212.53(Max Conc. mM)
- pka
- 12.85±0.70(Predicted)
- form
- Solid
- color
- Light yellow to yellow
N-Bromosuccinimide Price
- Product number
- CS-0030508
- Product name
- Poseltinib
- Purity
- 98.01%
- Packaging
- 5mg
- Price
- $190
- Updated
- 2021/12/16
- Product number
- CS-0030508
- Product name
- Poseltinib
- Purity
- 98.01%
- Packaging
- 10mg
- Price
- $320
- Updated
- 2021/12/16
- Product number
- CS-0030508
- Product name
- Poseltinib
- Purity
- 98.01%
- Packaging
- 50mg
- Price
- $800
- Updated
- 2021/12/16
- Product number
- DC11914
- Product name
- Poseltinib
- Purity
- >98%
- Packaging
- 100mg
- Price
- $800
- Updated
- 2021/12/16
Poseltinib Chemical Properties,Usage,Production
Uses
Poseltinib (HM71224) is an orally active, selective, irreversible small molecule Bruton tyrosine kinase (BTK) inhibitor. With an IC50 of 1.95 nM. Poseltinib effectively inhibits the signaling mediated by B cell receptors (BCR), Fc receptors (FcR), and Toll-like receptors (TLR). Poseltinib has anti-inflammatory activity and can be used in the research of rheumatoid arthritis[1][2][3].
in vivo
Poseltinib (3,-30 mg/kg, p.o, once a day, from 18 to 40 weeks) reduces the overactivity of B cells by inhibiting BTK, alleviating the development of systemic lupus erythematosus (SLE) and lupus nephritis (LN)[1].
Poseltinib (1-30 mg/kg p.o, once a day for 2 weeks) improves experimental arthritis in mice [2].
| Animal Model: | MRL/lpr mice and NZB/W F1 mice models[1] |
| Dosage: | 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[2] |
| 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. |
IC 50
TLRs
References
[1] Kim YY, et al. HM71224, a selective Bruton's tyrosine kinase inhibitor, attenuates the development of murine lupus. Arthritis Res Ther. 2017 Sep 26;19(1):211. DOI:10.1186/s13075-017-1402-1
[2] Park JK, et al. HM71224, a novel Bruton's tyrosine kinase inhibitor, suppresses B cell and monocyte activation and ameliorates arthritis in a mouse model: a potential drug for rheumatoid arthritis. Arthritis Res Ther. 2016 Apr 18;18:91. DOI:10.1186/s13075-016-0988-z
[3] Byun JY, et al. Target modulation and pharmacokinetics/pharmacodynamics translation of the BTK inhibitor poseltinib for model-informed phase II dose selection. Sci Rep. 2021 Sep 21;11(1):18671. DOI:10.1038/s41598-021-98255-7
Poseltinib Preparation Products And Raw materials
Raw materials
Preparation Products
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