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.
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- CAS No.: 1221878-06-3
- 화학식: C28H25F2N5O3
- 분자량:517.53
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
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] |
Chemical Information
-
CAS No. 1221878-06-3
-
분자량 517.53
-
화학식 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
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)