LOXO-292

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LOXO-292（Selpercatinib、LOXO 292、LOXO292）是一种有效的、选择性的、口服的 RET 激酶抑制剂，具有潜在的抗肿瘤活性。

LOXO-292 (Selpercatinib, LOXO 292, LOXO292) is a potent, selective, orally available RET kinase inhibitor with potential antineoplastic activity; displays >100-fold selectivity versus important off-targets; shows anti-tumor activty in the brain and periphery in RET-dependent tumor models in vivo.Lung Cancer Phase 1 Clinical(In Vivo):Selpercatinib (LOXO-292; 10 mg/kg; i.g.; for 0-2 h) has good pharmacokinetics after oral gavage in FVB/NRj mice.

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Selpercatinib (LOXO-292; 10 mg/kg; i.g.; for 0-2 h) has good pharmacokinetics after oral gavage in FVB/NRj mice.Pharmacokinetic Parameters of Selpercatinib in FVB/NRj mice.FVB/NRj mice, 10 mg/kg i.g. Animal Model:Male FVB/NRj mice Dosage:10 mg/kg Administration:Oral gavage; for 7.5 min, 15 min, 30 min, 1 h and 2 h (Pharmacokinetic Analysis)Result:Had good pharmacokinetics after oral gavage in FVB/NRj mice.

Selpercatinib | LOXO 292 | LOXO292

Tyrosine Kinase

c-RET

c-RET

Cancer

Lung Cancer

2152628-33-4

525.613

C29H31N7O3

>98% (HPLC)

DMSO : 8.33 mg/mL 15.85 mM

N#CC1=C2C(C3=CC=C(N4CC(C5)N(CC6=CC=C(OC)N=C6)C5C4)N=C3)=CC(OCC(C)(O)C)=CN2N=C1

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

(-20℃)

With Ice Pack

≥ 2 years