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RET-IN-13

Names

[ CAS No. ]:
2684258-54-4

[ Name ]:
RET-IN-13

Biological Activity

[Description]:

RET-IN-13 (compound 1), a quinoline compound, is a potent RET inhibitor with IC50s of 0.5 nM, 0.9 nM for RET (WT) and RET (V804M), respectively. RET-IN-13 has the potential for tumors or intestinal diseases related to abnormal activation of RET research[1].

[Related Catalog]:

Research Areas >> Cancer

[In Vitro]

RET-IN-13 has low inhibition on CYP1A2 (IC50>50 μM), CYP2C9 (IC50=12.5 μM), CYP2C19 (IC50=16.9 μM), CYP2D6 (IC50=18.8 μM) and CYP3A4 (IC50>50 μM)[1].

[In Vivo]

RET-IN-13 (compound 1; 0.5 mpk; iv) has a T1/2 of 6.93 hours, a CL of 2.68 mL/min·kg, and a Vdss of 1.52 L/kg for male mice[1]. RET-IN-13 (2.5 mpk; po) has a T1/2 of 5.16 hours, Cmax of 0.958 μM and an AUC of 12477 μM·hr for male mice[1].

[References]

[1]. Jiansong Wang, et al. Quinoline compounds. WO2021164742A1.

Chemical & Physical Properties

[ Molecular Formula ]:
C32H33F4N5O3

[ Molecular Weight ]:
611.63


Related Compounds