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Pirtobrutinib

Catalog No. T36287Cas No. 2101700-15-4

Pirtobrutinib (LOXO-305) is an advanced BTK inhibitor that displays high selectivity and operates through a non-covalent mechanism. This compound effectively inhibits various BTK C481 substitution mutations, leading to tumor regression in BTK-dependent lymphoma tumors in mouse xenograft models. Furthermore, Pirtobrutinib exhibits remarkable selectivity for BTK, with more than a 300-fold difference compared to 370 other kinases tested. Notably, at a concentration of 1 μM, Pirtobrutinib demonstrates no significant inhibition of non-kinase off-targets.

Pirtobrutinib

Pirtobrutinib

Purity: 99.89%
Catalog No. T36287Cas No. 2101700-15-4
Pirtobrutinib (LOXO-305) is an advanced BTK inhibitor that displays high selectivity and operates through a non-covalent mechanism. This compound effectively inhibits various BTK C481 substitution mutations, leading to tumor regression in BTK-dependent lymphoma tumors in mouse xenograft models. Furthermore, Pirtobrutinib exhibits remarkable selectivity for BTK, with more than a 300-fold difference compared to 370 other kinases tested. Notably, at a concentration of 1 μM, Pirtobrutinib demonstrates no significant inhibition of non-kinase off-targets.
Pack SizePriceAvailabilityQuantity
1 mg$31In Stock
5 mg$72In Stock
10 mg$128In Stock
25 mg$297In Stock
50 mg$457In Stock
100 mg$672In Stock
500 mg$1,4306-8 weeks
1 mL x 10 mM (in DMSO)$76In Stock
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Purity:99.89%
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Product Introduction

Bioactivity
Description
Pirtobrutinib (LOXO-305) is an advanced BTK inhibitor that displays high selectivity and operates through a non-covalent mechanism. This compound effectively inhibits various BTK C481 substitution mutations, leading to tumor regression in BTK-dependent lymphoma tumors in mouse xenograft models. Furthermore, Pirtobrutinib exhibits remarkable selectivity for BTK, with more than a 300-fold difference compared to 370 other kinases tested. Notably, at a concentration of 1 μM, Pirtobrutinib demonstrates no significant inhibition of non-kinase off-targets.
In vitro
Pirtobrutinib potently inhibits both wild-type BTK and BTK C481S-mediated kinase activity with nanomolar potency. Pirtobrutinib strongly inhibits WT BTK (Y223) autophosphorylation with an IC50 of 3.68 nM. Pirtobrutinib inhibits BTK C481S Y223, C481T Y223, and C481R Y223 autophosphorylation with IC50s of 8.45, 7.23, and 11.73 nM, respectively[1].
Chemical Properties
Molecular Weight479.43
FormulaC22H21F4N5O3
Cas No.2101700-15-4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 55 mg/mL (114.72 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0858 mL10.4291 mL20.8581 mL104.2905 mL
5 mM0.4172 mL2.0858 mL4.1716 mL20.8581 mL
10 mM0.2086 mL1.0429 mL2.0858 mL10.4291 mL
20 mM0.1043 mL0.5215 mL1.0429 mL5.2145 mL
50 mM0.0417 mL0.2086 mL0.4172 mL2.0858 mL
100 mM0.0209 mL0.1043 mL0.2086 mL1.0429 mL

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