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Poseltinib

Cat. No. M11431
Poseltinib Structure
Synonym:

HM71224; LY3337641

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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Poseltinib is an orally active, selective, irreversible small-molecule Bruton tyrosine kinase (BTK) inhibitor with an IC50 of 1.95 nM and 0.3, 2.3, and 2.4 fold selective action against BMX, TEC, and TXK, respectively. Poseltinib covalently binds to the active site of BTK (cysteine 481 residue) and effectively inhibits B cell receptor (BCR), Fc receptor (FcR), and Toll-like receptor (TLR) mediated signaling.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 470.52
Formula C26H26N6O3
CAS Number 1353552-97-2
Purity >98%
Solubility DMSO ≥ 60 mg/mL
Storage at -20°C
Related BTK Products
Vecabrutinib

Vecabrutinib (SNS-062) is a potent, non-covalent BTK and ITK inhibitor,Kd The values are 0.3 nM and 2.2 nM, respectively. Vecabrutinib for ITK IC50 The value is 24 nM.

Rilzabrutinib

Rilzabrutinib, also known as PRN1008, is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK) with IC50 of 1.3 nM.

Pirtobrutinib (LOXO-305)

Pirtobrutinib (LOXO-305; LY 3527727; RXC-005) is a highly selective and non-covalent next generation BTK inhibitor, which inhibits diverse BTK C481 substitution mutations. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases.

Remibrutinib (LOU064)

Remibrutinib (LOU064) is a potent and highly selective covalent Inhibitor of Bruton's Tyrosine Kinase (BTK) with IC50 value of 1 nM.

Tolebrutinib

Tolebrutinib (SAR442168) is a potent, selective, orally active and blood-brain barrier capable bruton's tyrosine kinase (BTK) inhibitor with IC50 values of 0.4 and 0.7 nM in Ramos B cells and HMC microglia, respectively. Tolebrutinib has an effect on central nervous system immunity. Tolebrutinib can be used in multiple sclerosis (MS) studies.

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Keywords: Poseltinib, HM71224; LY3337641 supplier, BTK, inhibitors

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