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Technical Data
| Formula | C17H12Cl2F3N7O2S |
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| Molecular Weight | 506.29 | CAS No. | 1096708-71-2 | |
| Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (197.51 mM) | |
| Ethanol | 13 mg/mL (25.67 mM) | |||
| Water | Insoluble | |||
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* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Preparing Stock Solutions
Biological Activity
| Description | Tovorafenib (MLN2480, BIIB-024, TAK580, AMG-2112819, BSK1369, DAY-101) is an oral, selective pan-Raf kinase inhibitor in chinical trials. | |
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| In vitro | MLN2480 inhibits MAPK pathway signaling in BRAF mutant and some RAS mutant preclinical cancer models at concentrations that are tolerated in vivo[1]. It is found to activate phosphorylated MEK at very low concentrations, but inhibits this same activity at higher concentrations. The inhibitory effects of MLN-2480 are found to vary across models and genetic contexts[2]. In vitro analysis of this drug combination of MLN2480 and TAK-733(an investigational allosteric MEK kinase inhibitor) in cell proliferation assays demonstrates synergistic activity .In addition, western blot analysis demonstrates the effect of MLN2480 in reversing feedback activation of MEK in response to TAK-733, leading to more concerted MAPK pathway inhibition.MLN-2480 only modestly inhibits PRAK[1][2]. |
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| In vivo | In vivo, MLN2480 shows antitumor activity in melanoma, colon, lung, and pancreatic cancer xenograft models[3]. 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 produces negligible effects[2]. |
Protocol (from reference)
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References
Selleck's Tovorafenib (MLN2480) has been cited by 6 publications
| BRAFΔβ3-αC in-frame deletion mutants differ in their dimerization propensity, HSP90 dependence, and druggability [ Sci Adv, 2023, 9(35):eade7486] | PubMed: 37656784 |
| Anti-tumor activity of the pan-RAF inhibitor TAK-580 in combination with KPT-330 (selinexor) in multiple myeloma [ Int J Hematol, 2021, 10.1007/s12185-021-03244-1] | PubMed: 34741230 |
| Genetic Heterogeneity of BRAF Fusion Kinases in Melanoma Affects Drug Responses. [ Cell Rep, 2019, 29(3):573-588] | PubMed: 31618628 |
| Development of Highly Sensitive Biosensors of RAF Dimerization in Cells. [ Sci Rep, 2019, 9(1):636] | PubMed: 30679688 |
| Comparative analysis of the phototoxicity induced by BRAF inhibitors and alleviation through antioxidants. [ Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520] | PubMed: 31618797 |
| Establishment and application of a novel patient-derived KIAA1549:BRAF-driven pediatric pilocytic astrocytoma model for preclinical drug testing [ Oncotarget, 2017, 8(7):11460-11479] | PubMed: 28002790 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.