XL541
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1221878-06-3
- 分子式: C28H25F2N5O3
- 分子量:517.53
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 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] |
| 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] |
化学情報
-
CAS 番号 1221878-06-3
-
分子量 517.53
-
分子式 C28H25F2N5O3
-
SMILES
FC1=CC=C(OC2=CC=C(NC([C@H]3N(C(CN4C=CN=N4)=O)C[C@H](CC5=CC=C(F)C=C5)C3)=O)C=C2)C=C1
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)