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CAS No.: 1437321-24-8

CEP-40783 Catalog No. CSN22558

Synonyms: RXDX-106

RXDX-106 inhibits TAM and c-MET phosphorylation in vitro. This inhibition of TAM and c-MET activation in vitro is accompanied by a decrease in downstream MAPK and PI3K signaling and cell viability. It completely inhibits cellular proliferation and viability at sub-nanomolar concentrations in TAM-expressing cells.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述RXDX-106 is a potent and selective type II pseudo-irreversible (slow off-rate) inhibitor of TYRO3, AXL, MER and c-MET, with IC50 values of 3.50nM, 0.69nM, and 1.89nM for TYRO3, AXL, and MER, respectively. It blocked TAM RTKs on both tumor and immune cells, both in vitro and in vivo. Oral administration of RXDX-106 at 30mg/kg, q.d., significantly promoted TGI in immunocompetent mice but not immunodeficient mice. It directly activated macrophages, leading to activation of NK and T cells, restoring tumor immunity. RXDX-106 significantly inhibited the growth of MerTK activated SNU-638 cells with decreased p-MerTK, p-ERK and p-AKT observed at concentration of 1μM post 1-6h treatment.
作用机制ATP-competitive inhibitor that targets all three TAM receptors.
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03454243	Advanced or Metastatic Solid T... more >>umors Collapse <<	Early Phase 1	Terminated(Sponsor's decision)	-	United States, Texas ... more >> START San Antonio, Texas, United States, 78229 Collapse <<

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.6991 mL
- 8.4953 mL
- 16.9907 mL
- 5 mM
- 0.3398 mL
- 1.6991 mL
- 3.3981 mL
- 10 mM
- 0.1699 mL
- 0.8495 mL
- 1.6991 mL

技术信息

CAS号

1437321-24-8

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C31H26F2N4O6

运输

蓝冰

分子量

588.56

别名

RXDX-106

溶解度

DMSO	10.0 mg/mL (17.0 mM)
Water	Insoluble
Ethanol	2.0 mg/mL (3.4 mM)

动物实验配方

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