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| Size | Price | Stock |
|---|---|---|
| 500mg | $500 | Check With Us |
| 1g | $880 | Check With Us |
| 5g | $1485 | Check With Us |
: Cat #: V0071 CAS #: 835621-07-3 Purity ≥ 98%
Description: Regorafenib HCl, the hydrochloric acid salt of regorafenib (also known as BAY 73-4506), is a potent inhibitor of multi-kinase including VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 values of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively.
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| Molecular Weight (MW) | 519.28 |
|---|---|
| Molecular Formula | C₂₁H₁₆Cl₂F₄N₄O₃ |
| CAS No. | 835621-07-3 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: >100 mg/mL (200.9 mM)r |
| Water: N/Ar | |
| Ethanol: N/A | |
| Solubility In Vivo | 30% PEG400+0.5% Tween80+5% Propylene glycol: 30mg/mL |
| SMILES Code | O=C(NC1=CC=C(C(C(F)(F)F)=C1)Cl)NC2=CC=C(OC3=CC(C(NC)=O)=NC=C3)C=C2F.O |
| Synonyms | BAY 73-4506 hydrochloride); Regorafenib Hydrochlorid; Regorafenib HCl |
| Protocol | 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. |
|---|---|---|
| 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. |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.9257 mL | 9.6287 mL | 19.2574 mL | 38.5149 mL |
| 5mM | 0.3851 mL | 1.9257 mL | 3.8515 mL | 7.7030 mL |
| 10mM | 0.1926 mL | 0.9629 mL | 1.9257 mL | 3.8515 mL |
| 20mM | 0.0963 mL | 0.4814 mL | 0.9629 mL | 1.9257 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.