1. PROTAC Protein Tyrosine Kinase/RTK Neuronal Signaling
  2. PROTACs Trk Receptor
  3. NTRK degrader-1

NTRK degrader-1 是一种可靶向野生型及突变型 (G595R、G667C、F598L) NTRK1PROTAC 降解剂与激酶抑制剂,其针对野生型、G595R、G667C、F598L 突变型的 IC50 值分别为 4 nM、2 nM、5 nM 及 <0.5 nM。NTRK degrader-1 可催化野生型及突变型 (G595R、G667C、F598L) NTRK1 的泛素化修饰及后续的蛋白酶体介导降解。NTRK degrader-1 可用于实体肿瘤的研究。

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NTRK degrader-1

NTRK degrader-1 Chemical Structure

CAS No. : 2922274-35-7

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生物活性

NTRK degrader-1 is a wild-type and mutant NTRK1 PROTAC degrader with IC50 values of 4 nM (wild-type), 2 nM (G595R), 5 nM (G667C), and <0.5 nM (F598L). NTRK degrader-1 catalyzes ubiquitination and subsequent proteasome-mediated degradation of wild-type and mutant (G595R, G667C, F598L) NTRK1.NTRK degrader-1 can be used for the research of solid tumors[1].

体外研究
(In Vitro)

NTRK degrader-1 (compound 5b) (6 h) 在 293 T 细胞中于 6 h 内降解野生型 NTRK1、NTRK1G595R、NTRK1G667C 和 NTRK1F598L,其 IP (拐点) 值分别为 0.2 nM、1 nM、2 nM 和 0.2 nM[1]
NTRK degrader-1 抑制野生型 NTRK1、NTRK1G595R、NTRK1G667C 和 NTRK1F598L,其 IC50 值分别为 4 nM、2 nM、5 nM 和 <0.5 nM[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

药代动力学
(Parmacokinetics)
Species Dose Route CL T1/2 Vss
Mice[1] 0.5 mg/kg i.v. 62 mL/mg/kg 1.6 h 3.1 L/kg
分子量

746.75

Formula

C38H35FN10O6

CAS 号
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.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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NTRK degrader-1
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HY-181052
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