Regorafenib hydrochlorideCAS# 835621-07-3 |
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Quality Control & MSDS
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| Cas No. | 835621-07-3 | SDF | Download SDF |
| PubChem ID | 66577009 | Appearance | Powder |
| Formula | C21H16Cl2F4N4O3 | M.Wt | 519.28 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | BAY73-4506 hydrochloride | ||
| Solubility | DMSO : ≥ 5.6 mg/mL (10.78 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide;hydrochloride | ||
| SMILES | CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F.Cl | ||
| Standard InChIKey | ACSWJKPZXNIVMY-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C21H15ClF4N4O3.ClH/c1-27-19(31)18-10-13(6-7-28-18)33-12-3-5-17(16(23)9-12)30-20(32)29-11-2-4-15(22)14(8-11)21(24,25)26;/h2-10H,1H3,(H,27,31)(H2,29,30,32);1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.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 nM[1]. 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[3].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[1]. References: | |||||
Regorafenib hydrochloride Dilution Calculator
Regorafenib hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.9257 mL | 9.6287 mL | 19.2574 mL | 38.5149 mL | 48.1436 mL |
| 5 mM | 0.3851 mL | 1.9257 mL | 3.8515 mL | 7.703 mL | 9.6287 mL |
| 10 mM | 0.1926 mL | 0.9629 mL | 1.9257 mL | 3.8515 mL | 4.8144 mL |
| 50 mM | 0.0385 mL | 0.1926 mL | 0.3851 mL | 0.7703 mL | 0.9629 mL |
| 100 mM | 0.0193 mL | 0.0963 mL | 0.1926 mL | 0.3851 mL | 0.4814 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf.
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Profile of trifluridine/tipiracil hydrochloride in the treatment of metastatic colorectal cancer: efficacy, safety, and place in therapy.[Pubmed:28979148]
Onco Targets Ther. 2017 Sep 15;10:4599-4605.
TAS-102, with its robust survival efficacy and feasible toxicity, is one of the standard salvage-line treatments for patients with metastatic colorectal cancer (mCRC). No definitive data are available to determine which drug should be administered first during salvage-line treatment. Therefore, it is imperative that we establish the sequence of administration by considering drug toxicity profiles based on patient characteristics, such as age, performance status, comorbidities, tolerability to previous treatments, and patient preferences. The identification of predictive biomarkers in response to TAS-102 or its toxicity is urgently needed for better patient selection. Moreover, to strengthen efficacy or relieve toxicity, combinations with other agents, which could potentially emerge as standard treatment regimens, have been investigated and compared to existing active regimens for mCRC.
Modulation of Regorafenib effects on HCC cell lines by epidermal growth factor.[Pubmed:25907508]
Cancer Chemother Pharmacol. 2015 Jun;75(6):1237-1245.
PURPOSE: Blood platelet numbers are correlated to growth and aggressiveness of several tumor types, including hepatocellular carcinoma (HCC). We previously found that platelet lysates (hPLs) also stimulated growth and migration, and antagonized the growth-inhibitory and apoptotic effects of both Sorafenib and Regorafenib, two multikinase inhibitors, on three HCC cell lines. In this study, in vitro function of human epidermal growth factor (EGF) with and without Sorafenib or Regorafenib was investigated. METHODS: An ELISA kit was used to evaluate the EGF concentrations in hPLs. In vitro function of EGF was assessed with proliferation MTT test. Apoptosis assay, scratch assays, and Transwell assays were performed for apoptosis, invasion, and migration, respectively. MAPK Activation Kit was used to explore MAPK phosphorylation. RESULTS: EGF antagonized the growth inhibition of Regorafenib on three HCC cell lines. Regorafenib-mediated growth inhibition was blocked by 70 % when the cells were pre-treated with EGF. EGF also blocked Regorafenib-induced apoptosis, as well as Regorafenib-induced decreases in cell migration and invasion. The EGF effects were in turn antagonized by concomitant addition to the cultures of EGF receptor antagonist Erlotinib, showing that the EGF receptor was involved in the mechanisms of EGF-mediated blocking of Regorafenib effects. Erlotinib also partially blocked the effects of hPLs in antagonizing Regorafenib-mediated growth inhibition, showing that EGF was an important component of hPL actions. CONCLUSIONS: All these results show that EGF antagonized Regorafenib-mediated growth and migration inhibition and apoptosis induction in HCC cells and reinforce the idea that microenvironment can influence cancer drug actions.
Elevated RET expression enhances EGFR activation and mediates EGFR inhibitor resistance in head and neck squamous cell carcinoma.[Pubmed:27090738]
Cancer Lett. 2016 Jul 10;377(1):1-10.
BACKGROUND AND AIM: Co-activation of EGFR by alternative receptor tyrosine kinases (RTKs) might mediate resistance to EGFR inhibition in head and neck squamous cell carcinoma (HNSCC). Here we found a novel mechanism to improve the efficacy of EGFR inhibitor erlotinib on HNSCC. METHOD: Immunohistochemistry, western blot, cell migration and invasion assays, cell proliferation, cell cycle analysis and in vivo serial transplantation assays were used to evaluate the role of RET on HNSCC cells. RESULTS: The elevated levels of a rearranged during transfection (RET) are observed in HNSCC and that high levels of RET correlate with increased tumor size, advanced tumor stage and decreased overall survival rate. The HNSCC cell proliferation and invasion were inhibited by RET knockdown in vitro and in vivo. The inhibition of RET expression markedly reduced EGFR phosphorylation and downstream EGFR signaling. The inhibition of RET signaling significantly increased the sensitivity of HNSCC cells to the EGFR inhibitor erlotinib in both in vitro and in vivo models. CONCLUSION: Our results offer a preclinical proof-of-concept supporting a role for RET signaling inhibition in a targeted therapeutic approach to improve the efficacy of EGFR inhibition in HNSCC.
TAS-102 for the treatment of metastatic colorectal cancer.[Pubmed:26509228]
Expert Rev Anticancer Ther. 2015;15(11):1283-92.
The survival of patients with metastatic colorectal cancer has notably increased in the past 20 years, from 12 months to around 30 months. Nevertheless, the prognosis of patients pretreated with all available agents is poor and there is high unmet need for newer treatments. TAS-102 is an orally administered combination of the nucleoside analogue trifluridine and tipiracil hydrochloride, a thymidine phosphorylase inhibitor. In a randomized trial of 800 patients who had received at least two other treatments previously (most patients had received more than four treatments). TAS-102 demonstrated a significant prolongation of overall survival compared with placebo (median survival 7.1 vs. 5.3 months; hazard ratio 0 . 68, 95%CI: 0 . 58-0 . 81; p < 0 . 001). The toxicity was manageable, grade 3 or higher events occurred in 69% of patients in the TAS-102 group versus 52% in the placebo group, with neutropenia the most common event.
Safety and Efficacy of Trifluridine/Tipiracil Monotherapy in Clinical Practice for Patients With Metastatic Colorectal Cancer: Experience at a Single Institution.[Pubmed:26723516]
Clin Colorectal Cancer. 2016 Sep;15(3):e109-15.
BACKGROUND: The combination drug TAS-102 is a novel oral nucleoside antitumor agent containing trifluridine and tipiracil hydrochloride, which prevents the degradation of trifluridine. The global phase III RECOURSE trial (Study of TAS-102 in Patients With Metastatic Colorectal Cancer Refractory to Standard Chemotherapies) demonstrated that TAS-102 prolonged the survival of patients with metastatic colorectal cancer (mCRC) whose disease progressed after standard therapies. TAS-102 was first approved in Japan in March 2014, and little is known about its safety and efficacy in clinical practice, especially for mCRC patients with previous regorafenib treatment. PATIENTS AND METHODS: We investigated the safety and efficacy of TAS-102 monotherapy in clinical practice for patients with mCRC refractory to standard therapies who were treated from May 2014 to January 2015. RESULTS: A total of 55 patients received TAS-102. The Eastern Cooperative Oncology Group performance status was 0, 1, and 2 in 41.8%, 47.3%, and 10.9% of patients. Of the 55 patients, 32 (58.2%) had been treated with regorafenib before receiving TAS-102. The median progression-free survival and overall survival was 2.0 months and 5.3 months, respectively. Emergency hospitalization was required for 23.6% of the patients during TAS-102 treatment, although most of the events (76.9%) were disease-related. The most common grade 3 or 4 adverse events were neutropenia (41.8%), leukopenia (27.2%), anemia (23.6%), febrile neutropenia (5.5%), and fatigue (3.6%). The frequency of grade >/= 3 events was not significantly increased among the patients who had compared with those who had not received regorafenib. The progression-free survival (median 2.1 vs. 2.0 months) and overall survival (median 6.2 vs. 4.7 months) were similar for the 2 subgroups. CONCLUSION: The safety and efficacy of TAS-102 monotherapy in clinical practice were maintained, irrespective of previous regorafenib treatment.
