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Pirtobrutinib

Chemical Structure : Pirtobrutinib

CAS No.: 2101700-15-4

Pirtobrutinib (LOXO-305, LOXO305, LY3527727, RXC-005)

Catalog No.: PC-72630Not For Human Use, Lab Use Only.

Pirtobrutinib (LOXO-305, LY3527727, RXC-005) is a highly potent and selective non-covalent BTK inhibitor with IC50 of 5.69 nM, shows nanomolar potency against both wild-type and C481-mutated BTK.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Pirtobrutinib (LOXO-305, LY3527727, RXC-005) is a highly potent and selective non-covalent BTK inhibitor with IC50 of 5.69 nM.
LOXO-305 shows nanomolar potency against both wild-type and C481-mutated BTK.
LOXO-305 displays >300 fold selectivity on BTK over 98% of other kinases, reducing the potential for off-target toxicities.
Pirtobrutinib (LOXO-305) has been designed to maintain greater than 90% of maximal BTK inhibition at trough, thereby achieving effective target inhibition throughout the dosing interval, even in proliferative tumours.

Physicochemical Properties

M.Wt 479.436
Formula C22H21F4N5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-amino-3-[4-[[(5-fluoro-2-methoxybenzoyl)amino]methyl]phenyl]-1-[(2S)-1,1,1-trifluoropropan-2-yl]pyrazole-4-carboxamide

References

1. Brandhuber B, et al. Clin. Lymphoma Myeloma Leuk. 2018;18:S216.

2. Ito K, et al. Eur J Cancer. 2021 Mar;145:183-193.

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