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Selpercatinib

Chemical Structure : Selpercatinib

CAS No.: 2152628-33-4

Selpercatinib (LOXO-292, LOXO292)

Catalog No.: PC-60209Not For Human Use, Lab Use Only.

Selpercatinib (LOXO-292, LOXO292) is a potent, selective, orally available RET kinase inhibitor with IC50 of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively.

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

Biological Activity

Selpercatinib (LOXO-292, LOXO292) is a potent, selective, orally available RET kinase inhibitor with IC50 of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively.
LOXO-292 displays >100-fold selectivity versus important off-targets.
LOXO-292 shows anti-tumor activty in the brain and periphery in RET-dependent tumor models in vivo.

Physicochemical Properties

M.Wt 525.613
Formula C29H31N7O3
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

6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile

References

1. Subbiah V, et al. Ann Oncol. 2018 Aug 1;29(8):1869-1876.

2. Cancer Discov. 2018 Aug;8(8):904-905.

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