TRK-IN-21

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TRK-IN-21

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2429985-55-5

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

TRK-IN-21 (5n) 是一种具有口服活性的TRK抑制剂。TRK-IN-21 抑制 TRKA^WT，TRKA^G667C，TRKA^F589L和 TRKA^G595，其IC₅₀值分别为 0.3，2.3，0.4 和 0.5 nM。TRK-IN-21 可以用于癌症的研究。

生物活性

TRK-IN-21 (5n) is an orally activityTRKinhibitor. TRK-IN-21 inhibitsTRKA^WT,TRKA^G667C,TRKA^F589L, andTRKA^G595withIC₅₀s of 0.3, 2.3, 0.4 and 0.5 nM, respectively. TRK-IN-21 can be used for the research ofcancer^[1].

IC₅₀& Target

IC50: 0.3 nM (TRKA^WT), 2.3 nM (TRKA^G667C), 0.4 nM (TRKA^F589L), 0.5 nM (TRKA^G595)^[1]

体内研究
(In Vivo)

TRK-IN-21 (30-100 mg/kg; p.o. twice daily for 11-14 days) inhibits tumor growth in Ba/F₃-TRKA xenograft models^[1].
1.19Pharmacokinetic Properties of TRK-IN-21 in Rats and Dogs^[1].

	Rats IV 1 mg/kg	Rats IV 5 mg/kg	Dogs IV 2 mg/kg	Dogs PO 10 mg/kg
C_max(ng/mL)	231.2	93.5	1063.8	2070.1
T_max(h)	0.1	1.7		0.3
AUC_last(ng·h/mL)	456.1	588.6	6923.0	24305.2
CL (L/h/kg)	2.1	8.0	0.2	0.3
T_1/2(h)	2.2	2.2	15.2	15.3
Vz (L/kg)	6.7	25.7	4.2	6.2
MRT (h)	2.5	4.0	8.2	8.8
F (%)		26	30.2	71

Animal Model:	6-week-old BALB/cA nude mice with Ba/F₃-TRKA xenografts^[1]
Dosage:	30 and 100 mg/kg
Administration:	Oral gavage; 30 and 100 mg/kg twice daily; for 11-14 days
Result:	Dose-dependently inhibited BaF₃-TMP3-TRKA^WT-transfected tumor progression with a tumor growth inhibition value of 97%, showed a better potency to larotrectinib at the same dosage. Inhibited BaF₃-LMNA-TrkA^G667C-transfected tumor progression with a tumor growth inhibition value of 73%, showed a better potency to selitrectinib at the same dosage.

分子量

424.45

Formula

C₂₂H₂₂F₂N₆O

CAS 号

2429985-55-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.