TIY-7,2846435-83-2

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

TIY-7

CAS No. : 2846435-83-2

MCE 国际站：TIY-7

产品活性：TIY-7 是一种选择性和具有口服活性的 原肌球蛋白受体激酶 (TRK) 抑制剂。TIY-7 对 TRKA, TRKA^G595R, TRKA^G667C, TRKA^F589L, TRKC^G623R, TRKC^G696A 酶均显示出抑制活性其 IC₅₀ 值分别为 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM。TIY-7 在小鼠异种移植模型中显示出抗肿瘤效力。

研究领域：Neuronal Signaling  |  Protein Tyrosine Kinase/RTK

作用靶点：Trk Receptor

In Vitro: TIY-7 (compound 12c) shows enzyme inhibitory activity with IC₅₀s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKA^G595R, TRKA^G667C, TRKA^F589L, TRKC^G623R, TRKC^G696A, respectively.
TIY-7 (1 µM) shows selectivity with inhibitory rate of 62%, 99%, 11% for ALK, ROS1, and JAK1 kinase.

In Vivo: TIY-7 (5 mg/kg for p.o.; 1 mg/kg for i.v.) shows good oral bioavailability (F) of 39.8%.
TIY-7 (30 mg/kg; P.o.; twice daily for 12-14 consecutive days) inhibits tumor progression in a dose-dependent manner in xenograft model.
Pharmacokinetic Parameters of TIY-7 in Male Sprague-Dawley rats.

	Dose (mg/kg)	Cmax (ng/mL)	Tmax (h)	T1/2 (h)	CL (mL/min/kg)	F %	MRT0-t (h)	AUCtot (ng/mL·h)	AUCextra (%)
ip mice	9.103	2078	0.0833	0.8	154	86	0.7	982.3	1.3
iv mice	0.711	322.7	0.0833	1.1	133		0.9	88.8	15.2
iv dog	26.76	272 (µg/mL)	0.0833	3.8	0.69		3.8	654.7 (µg/mL·h)	0.9

Male Sprague-Dawley rats; 5 mg/kg for p.o.; 1 mg/kg for i.v..

相关产品：Entrectinib  |  Larotrectinib  |  ANA-12  |  7,8-Dihydroxyflavone  |  Repotrectinib  |  Sitravatinib  |  K-252a  |  Amitriptyline hydrochloride  |  GW 441756  |  GNF-5837  |  Lestaurtinib  |  Selitrectinib  |  N-Acetyl-5-hydroxytryptamine  |  LM22B-10  |  Altiratinib  |  AZ-23  |  Tyrphostin AG 879  |  Tamnorzatinib  |  Cyclotraxin B  |  LM22A-4  |  Tavilermide  |  Belizatinib  |  DS-1205b free base  |  TrkA-IN-1  |  PF-6683324  |  CH7057288  |  2-Bromo-6-methoxynaphthalene  |  GNF-8625 monopyridin-N-piperazine hydrochloride

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds