XL-281
XL-281 (BMS-908662) is an orally active inhibitor for RAF kinase, with IC50s of 2.6, 4.5 and 6 nM, for CRAF, B-RAF, and B-RAFV600E, respectively. XL-281 exhibits antitumor activity.
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- CAS No.: 870603-16-0
- Formule: C24H19ClN4O4
- Masse moléculaire:462.89
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
|
C-Raf 2.6 nM (IC50) |
B-Raf 4.5 nM (IC50) |
B-RafV600E 6 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SK-MEL19 | IC50 |
200 nM
Compound: 8; XL281; BMS-908662
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Cytotoxicity against human SK-MEL-19 cells harboring BRAF mutant after 3 days
Cytotoxicity against human SK-MEL-19 cells harboring BRAF mutant after 3 days
|
[PMID: 29461827] |
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 870603-16-0
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Masse moléculaire 462.89
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Formule C24H19ClN4O4
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SMILES
O=C(OC)NC1=NC2=CC=C(C3(O)N(C4=CC(Cl)=CC=C4C)C(C5=C3C=CC=C5)=O)C=C2N1
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Synonyms
BMS-908662
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)