1. GPCR/G Protein
  2. LPL Receptor
  3. XL541

XL541 是一种强效、选择性的 S1P1 拮抗剂。XL541 抑制 GDP-GTP 交换。XL541 可引起肿瘤表面明显出血。XL541 与 Paclitaxel (HY-B0015) 协同作用,对乳腺癌和肺癌表现出抗肿瘤活性。

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XL541

XL541 Chemical Structure

CAS No. : 1221878-06-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

XL541 is a potent, selective S1P1 antagonist. XL541 inhibits GDP-GTP exchange. XL541 causes frank surface hemorrhaging of tumors. XL541 collaborates with Paclitaxel (HY-B0015) to exhibit antitumor activity against breast cancer and lung cancer[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
26 nM
Compound: 37, XL541
Antagonist activity at S1P1 receptor expressed in HEK293 cells assessed as inhibition of S1P-induced tango beta-arrestin recruitment preincubated for 30 mins prior S1P addition measured after 16 to 18 hrs by luciferase reporter gene assay
Antagonist activity at S1P1 receptor expressed in HEK293 cells assessed as inhibition of S1P-induced tango beta-arrestin recruitment preincubated for 30 mins prior S1P addition measured after 16 to 18 hrs by luciferase reporter gene assay
[PMID: 22214363]
HEK293 IC50
5.8 nM
Compound: 37, XL541
Antagonist activity at S1P1 receptor expressed in HEK293 cells assessed as inhibition of S1P-induced cAMP response after 90 mins by spectrophotometry
Antagonist activity at S1P1 receptor expressed in HEK293 cells assessed as inhibition of S1P-induced cAMP response after 90 mins by spectrophotometry
[PMID: 22214363]
HEK293 IC50
> 10000 nM
Compound: 37, XL541
Antagonist activity at S1P2 receptor expressed in HEK293 cells assessed as inhibition of S1P-induced tango beta-arrestin recruitment preincubated for 30 mins prior S1P addition measured after 16 to 18 hrs by luciferase reporter gene assay
Antagonist activity at S1P2 receptor expressed in HEK293 cells assessed as inhibition of S1P-induced tango beta-arrestin recruitment preincubated for 30 mins prior S1P addition measured after 16 to 18 hrs by luciferase reporter gene assay
[PMID: 22214363]
HEK293 IC50
> 10000 nM
Compound: 37, XL541
Antagonist activity at S1P3 receptor expressed in HEK293 cells assessed as inhibition of S1P-induced tango beta-arrestin recruitment preincubated for 30 mins prior S1P addition measured after 16 to 18 hrs by luciferase reporter gene assay
Antagonist activity at S1P3 receptor expressed in HEK293 cells assessed as inhibition of S1P-induced tango beta-arrestin recruitment preincubated for 30 mins prior S1P addition measured after 16 to 18 hrs by luciferase reporter gene assay
[PMID: 22214363]
分子量

517.53

Formula

C28H25F2N5O3

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
  • 摩尔计算器

  • 稀释计算器

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× = ×
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Help & FAQs
  • 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:
XL541
目录号:
HY-18165
需求量: