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Formula | C21H16ClF3N4O3.C7H8O3S |
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Molecular Weight | 637.03 | CAS No. | 475207-59-1 | |
Solubility (25°C)* | In vitro | DMSO | 127 mg/mL (199.36 mM) | |
Water | 0.01 mg/mL (0.01 mM) | |||
Ethanol | Insoluble | |||
* <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.) |
Description | Sorafenib tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity. | |||||||||||
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In vitro | Sorafenib tosylate inhibits both wild-type and V599E mutant B-Raf activity with IC50 of 22 nM and 38 nM, respectively. Sorafenib tosylate also potently inhibits mVEGFR2 (Flk-1), mVEGFR3, mPDGFRβ, Flt3, and c-Kit with IC50 of 15 nM, 20 nM, 57 nM, 58 nM, and 68 nM, respectively. Sorafenib tosylate weakly inhibits FGFR-1 with IC50 of 580 nM. Sorafenib tosylate is not active against ERK-1, MEK-1, EGFR, HER-2, IGFR-1, c-Met, PKB, PKA, cdk1/cyclinB, PKCα, PKCγ, and pim-1. Sorafenib tosylate markedly inhibits VEGFR2 phosphorylation in NIH 3T3 cells with IC50 of 30 nM, and Flt-3 phosphorylation in HEK-293 cells with IC50 of 20 nM. Sorafenib tosylate potently blocks MEK 1/2 and ERK 1/2 phosphorylation in most cell lines but not in A549 or H460 cells, while having no effect on inhibition of the PKB pathway. Sorafenib tosylate inhibits the proliferation of HAoSMC and MDA-MB-231 cells with IC50 of 0.28 μM and 2.6 μM, respectively. [1] In addition to inhibition of the RAF/MEK/ERK signaling pathway, Sorafenib tosylate significantly inhibits the phosphorylation of eIF4E and down-regulates Mcl-1 levels in hepatocellular carcinoma (HCC) cells in a MEK/ERK-independent manner. Sorafenib tosylate inhibits the proliferation of PLC/PRF/5 and HepG2 cells with IC50 of 6.3 μM and 4.5 μM, respectively, and leads to the significant induction of apoptosis. [2] |
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In vivo | Oral administration of Sorafenib tosylate (~60 mg/kg) demonstrates broad spectrum, dose-dependent anti-tumor activity against a variety of human tumor xenograft models including MDA-MB-231, Colo-205, HT-29, DLD-1, NCI-H460, and A549, with no evidence of toxicity. In association with the anti-tumor efficacy, Sorafenib tosylatetreatment potently inhibits MEK 1/2 phosphorylation and pERK 1/2 levels in HT-29 and MDA-MB-231 xenografts but not in Colo-205 xenografts, and significantly suppresses tumor microvessel area (MVA) and microvessel density (MVD) in MDA MB-231, HT-29 and Colo-205 tumor xenografts. [1] Sorafenib tosylate treatment produces dose-dependent growth inhibition of PLC/PRF/5 tumor xenografts in SCID mice with TGIs of 49% and 78% at 10 mg/kg and 30 mg/kg, respectively, consistent with the inhibition of ERK and eIF4E phosphorylation, reduction of the microvessel area, and induction of tumor cell apoptosis. [2] |
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, 2013, Christina W Yde/CDM Danish Cancer Society Research Center Denmark
Data from [Surgery, 2012, 152(6), 1142-9]
Data from [Surgery, 2012, 152(6), 1142-9]
Data from [J Invest Dermatol, 2011, 131, 1886–1895]
Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer [ Nature, 2024, 629(8013):927-936] | PubMed: 38588697 |
Targeting NG2 relieves the resistance of BRAF-mutant thyroid cancer cells to BRAF inhibitors [ Cell Mol Life Sci, 2024, 81(1):238] | PubMed: 38795180 |
Mitochondrial GCN5L1 acts as a novel regulator for iron homeostasis to promote sorafenib sensitivity in hepatocellular carcinoma [ J Transl Med, 2024, 22(1):593] | PubMed: 38918793 |
IL-22 signaling promotes sorafenib resistance in hepatocellular carcinoma via STAT3/CD155 signaling axis [ Front Immunol, 2024, 15:1373321] | PubMed: 38596684 |
EZH2 suppresses ferroptosis in hepatocellular carcinoma and reduces sorafenib sensitivity through epigenetic regulation of TFR2 [ Cancer Sci, 2024, 115(7):2220-2234] | PubMed: 38623968 |
Upregulation of LHPP by saRNA inhibited hepatocellular cancer cell proliferation and xenograft tumor growth [ PLoS One, 2024, 19(5):e0299522] | PubMed: 38696452 |
Gravitational and mechanical forces drive mitochondrial translation [ bioRxiv, 2024, 10.1101/2023.01.18.524628] | PubMed: none |
Arginine reprograms metabolism in liver cancer via RBM39 [ Cell, 2023, 186(23):5068-5083.e23] | PubMed: 37804830 |
Arginine reprograms metabolism in liver cancer via RBM39 [ Cell, 2023, S0092-8674(23)01032-2] | PubMed: 37804830 |
QKI shuttles internal m7G-modified transcripts into stress granules and modulates mRNA metabolism [ Cell, 2023, 186(15):3208-3226.e27] | PubMed: 37379838 |
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