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Tolebrutinib

Cat. No. M10274
Tolebrutinib Structure
Synonym:

SAR442168; PRN2246

Size Price Availability Quantity
10mg USD 432  USD480 In stock
50mg USD 1152  USD1280 In stock
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Quality Control
  • Current batch:
  • Purity >98.5%
  • COA
  • MSDS
Biological Activity

Tolebrutinib, also known as SAR442168, is a Bruton tyrosine kinase (BTK) inhibitor, with IC50 values of 0.4 nM and 0.7 nM in Ramos B cells and HMC microglia cells, respectively. Tolebrutinib blocks the BCR-mediated activation (IC50=10 nM) and Fc receptor activation (IC50=166 and 9.6 nM for FcεR and FcγR, repectively) of immune cells. Tolebrutinib inhibits microglial FcγR activation through durable occupancy of BTK, with an IC50 of 157 nM.

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 455.51
Formula C26H25N5O3
CAS Number 1971920-73-6
Purity >98.5%
Solubility DMSO 80 mg/mL
Storage at -20°C
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Remibrutinib (LOU064) is a potent and highly selective covalent Inhibitor of Bruton's Tyrosine Kinase (BTK) with IC50 value of 1 nM.

Orelabrutinib

Orelabrutinib is an orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK).

Zanubrutinib

Zanubrutinib (BGB-3111) is a potent and highly selective small molecule inhibitor of Bruton's tyrosine kinase (BTK).

ARQ 531

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Tolebrutinib, SAR442168; PRN2246 supplier, BTK, inhibitors

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