| Identification | Back Directory | [Name]
Regorafenib (Hydrochloride) | [CAS]
835621-07-3 | [Synonyms]
Regafenib HCL
Regorafenib HC
Regorafenib HCl
Regafenib hydrochloride
BAY73-4506 hydrochloride
Regorafenib (Hydrochloride)
Regorafenib HCl (BAY-73-4506)
Powder Regorafenib Hydrochloride CAS
Regorafenib Hydrochloride/BAY73-4506 hydrochloride
4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide hydr
4-[4-[[4-Chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide hydrochloride
4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrochloride (1:1)
4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrochloride
2-Pyridinecarboxamide,4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-, monohydrochloride | [EINECS(EC#)]
692-722-3 | [Molecular Formula]
C21H16Cl2F4N4O3 | [MDL Number]
MFCD22417053 | [MOL File]
835621-07-3.mol | [Molecular Weight]
519.276 |
| Chemical Properties | Back Directory | [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 | [color ]
White to off-white |
| Hazard Information | Back Directory | [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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