1. Protein Tyrosine Kinase/RTK
  2. TAM Receptor
  3. UNC3133

UNC3133 (Compound 16) 是一种选择性且具有口服活性的大环 Mer 酪氨酸激酶 (MerTK) 抑制剂,其 IC50 为 8.1 nM。UNC3133 对 TAM 家族 (AxlTyro3) 具有一定的选择性 (对 Axl 的选择性约为 7 倍,对 Tyro3 的选择性约为 10 倍),并且对 Flt3 具有相似的抑制活性。UNC3133 具有抗肿瘤和抗感染活性。

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UNC3133

UNC3133 Chemical Structure

CAS No. : 2011034-35-6

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  • 生物活性

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生物活性

UNC3133 (Compound 16) is a selective and orally active macrocyclic mer tyrosine kinase (MerTK) inhibitor with an IC50 of 8.1 nM. UNC3133 has certain selectivity towards the TAM family (Axl and Tyro3) (with a selectivity of approximately 7 times for Axl and about 10 times for Tyro3), and has similar inhibitory activity towards Flt3. UNC3133 exhibits anti-tumor and anti-infection activities[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
110 nM
Compound: 16
Inhibition of human MerTK kinase domain (1585 to 3000 residues) expressed in HEK293 cells co-expressing rat EGFR LBD assessed as inhibition of EGF-stimulated MerTK phosphorylation preincubated for 30 mins followed by EGF stimulation for 15 mins by ELISA
Inhibition of human MerTK kinase domain (1585 to 3000 residues) expressed in HEK293 cells co-expressing rat EGFR LBD assessed as inhibition of EGF-stimulated MerTK phosphorylation preincubated for 30 mins followed by EGF stimulation for 15 mins by ELISA
[PMID: 27994735]
分子量

504.71

Formula

C30H44N6O

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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  • 稀释计算器

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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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产品名称:
UNC3133
目录号:
HY-115778
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