Antibodies
MLN2480
- 貨號 Cat. No.
- S7121
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
MLN2480
Catalog No.S7121
MLN-2480 (BIIB-024) is a pan-Raf inhibitor.
| Availability |
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Biological Activity
| Description | MLN-2480 (BIIB-024) is a pan-Raf inhibitor. | |||||
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| Targets | ||||||
| IC50 | ||||||
| In vitro | MLN-2480 is active against wild-type B-raf and B-raf Val600Glu in vitro. MLN-2480 is found to activate phosphorylated MEK at very low concentrations, but at higher concentrations MLN-2480 inhibits this same activity. MLN-2480 inhibits signaling pathway at high concentrations in the human malignant melanoma A-375 mutant B-raf Val600Glu cell line. The inhibitory effects of MLN-2480 are found to vary across models and genetic contexts; MLN-2480 only modestly inhibits PRAK. MLN-2480 in combination with TAK-733 demonstrates synergy in NRAS mutant human malignant melanoma cell lines (SK-MEL-2), with high levels of apoptotic biomarkers observed. [1] | |||||
| In vivo | MLN-2480 (37.5 mg/kg) is well tolerated in a tumor xenograft model. The combination of MLN-2480 (12.5 mg) and TAK-733 (1 mg/kg) is effective in an SK-MEL-30 xenograft model, but monotherapy with either compound produced negligible effects. [1] | |||||
| Features | ||||||
Protocol(Only for Reference)
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01425008 | Recruiting | Melanoma|Metastatic Melanoma|Solid Tumor | Millennium Pharmaceuticals, Inc. | 2011-09 | Phase 1 |
Chemical Information
| Molecular Weight (MW) | 506.29 |
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| Formula | C17H12Cl2F3N7O2S |
| CAS No. | 1096708-71-2 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | BIIB-024 |
| Solubility (25°C) * | In vitro | DMSO | mg/mL (<1 mM) |
|---|---|---|---|
| Water | mg/mL (<1 mM) | ||
| Ethanol | mg/mL (<1 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 4-Pyrimidinecarboxamide, 6-amino-5-chloro-N-[(1R)-1-[5-[[[5-chloro-4-(trifluoromethyl)-2-pyridinyl]amino]carbonyl]-2-thiazolyl]ethyl]- |
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