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| | Regorafenib (Hydrochloride) Basic information |
| Product Name: | Regorafenib (Hydrochloride) | | Synonyms: | BAY73-4506 hydrochloride;4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrochloride;Regafenib HCL;Regafenib hydrochloride;2-Pyridinecarboxamide,4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-, monohydrochloride;4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrochloride (1:1);4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide hydr;Regorafenib (Hydrochloride) | | CAS: | 835621-07-3 | | MF: | C21H16Cl2F4N4O3 | | MW: | 519.2763528 | | EINECS: | 692-722-3 | | Product Categories: | | | Mol File: | 835621-07-3.mol |  |
| | Regorafenib (Hydrochloride) Chemical Properties |
| storage temp. | Store at -20°C | | solubility | ≥ 25.95 mg/mL in DMSO, ≥ 8.75 mg/mL in EtOH with ultrasonic and warming | | form | Powder |
| | Regorafenib (Hydrochloride) Usage And Synthesis |
| Uses | BAY 73-4506 (Regorafenib) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. | | in vitro | Regorafenib potently inhibits VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with an IC50 of 3 nM. In HAoSMCs, regorafenib inhibits PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM. Regorafenib inhibits the proliferation of VEGF165-stimulated HUVECs, with an IC50 of 3 nMf. Regorafenib causes a concentration-dependent decrease in Hep3B cell growth, having an IC50 of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells.
| | in vivo | Regorafenib effectively inhibits growth of the Colo-205 xenografts in the dose range of 10-100 mg/kg reaching a TGI of 75% at day 14 at the 10 mg/kg dose. In the MDA-MB-231 model, regorafenib is highly efficacious at a dose as low as 3 mg/kg, resulting in a significant TGI of 81%, which increases to 93% at doses of 10 and 30 mg/kg, where tumor stasis is reached. | | References | [1] Phan, Chiuyen et al. “Isomorphous Crystals Formed by the Similar Supramolecular Motifs in Sorafenib Hydrochloride and Regorafenib Hydrochloride Salts.” 2019. 0.
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| | Regorafenib (Hydrochloride) Preparation Products And Raw materials |
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