LOXO-292 Chemical Properties

Density 

1.36±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO:20.0(Max Conc. mg/mL);38.05(Max Conc. mM)

form 

A crystalline solid

pka

14.00±0.29(Predicted)

color 

White to off-white

InChI

InChI=1S/C29H31N7O3/c1-29(2,37)18-39-24-9-25(28-21(10-30)13-33-36(28)17-24)20-5-6-26(31-12-20)34-15-22-8-23(16-34)35(22)14-19-4-7-27(38-3)32-11-19/h4-7,9,11-13,17,22-23,37H,8,14-16,18H2,1-3H3

InChIKey

XIIOFHFUYBLOLW-UHFFFAOYSA-N

SMILES

C12=C(C#N)C=NN1C=C(OCC(O)(C)C)C=C2C1=CC=C(N2CC3CC(N3CC3=CC=C(OC)N=C3)C2)N=C1

LOXO-292 Usage And Synthesis

Binding Mode

In the co-crystal structure of selpercatinib-RET kinase, the pyrazolopyridine occupies the adenosine pocket, forming a direct hydrogen bond between N1 and amide NH of Ala807 and an indirect hydrogen bond between C6 ether oxygen and amide NH of Gly810 via a bound water molecule. In addition, one piperazine nitrogen also interact with one water molecule (Figs. 3, 4).

Uses

Selpercatinib is a highly selective, potent RET inhibitor, an oral drug used to treat cancers in people whose tumours have been altered (mutated or fused) in specific genes (RET stands for "rearrangement during transfection").

brand name

Retevmo

General Description

Class: receptor tyrosine kinase; Treatment: RET-altered lung/thyroid cancers; Other name: ARRY-192, LOXO-292; Oral bioavailability = 73%; Elimination half-life = 32 h; Protein binding = 97%

Side effects

Selpercatinib can cause serious side effects including liver toxicity, high blood pressure, heart rhythm changes due to prolongation of heart electrical activity (QT prolongation), bleeding, allergic reactions, impaired wound healing and harm to an unborn baby.

Selpercatinib may cause harm to a developing fetus or a newborn baby.

target

RET

storage

Store at -20°C

Dosage

The recommended selpercatinib dose based on body weight is: (1) Less than 50 kg: 120 mg orally twice daily (2) 50 kg or greater: 160 mg orally twice daily

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