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| 5mg |
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| 25mg |
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Purity: ≥98%
Fruquintinib (formerly known as HMPL-013; Elunate; Fruzaqla) is a novel, potent, selective and oral small molecule inhibitor of VEGFR1/2/3 family (IC50s = 33, 0.35, and 35 nM) with strong potency and high selectivity. It is presently undergoing Phase II clinical trials and may have anti-angiogenic and anticancer properties. Frucquintinib's first worldwide approval for the treatment of metastatic colorectal cancer (CRC) in patients who have not responded to at least two systemic anti-neoplastic therapies was given in China in September 2018. Phase III clinical trials on fruquintinib are currently being conducted to treat advanced gastric cancer and non-small cell lung cancer. Fruquintinib (Fruzaqla) was approved in 2023 by FDA for treating Colorectal cancer.
| Targets |
VEGFR1 (IC50 = 33 nM); VEGFR2 (IC50 = 35 nM); VEGFR3 (IC50 = 0.5 nM)
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| Enzyme Assay |
Fruquintinib suppresses VEGF/VEGFR cell signaling in human umbilical vein endothelial cells (HUVEC) and human lymphatic endothial cells (HLEC) with an IC50 at low nanomolar level in in vitro enzymatic and cellular assays. Out of the 253 kinases tested, only a small number of them, besides VEGFRs, are inhibited. Fruquintinib is a highly potent inhibitor of angiogenesis induced by VEGF.
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| Cell Assay |
In flat-bottomed 96-well plates, 100 mL of media containing 0.5% foetal bovine serum (FBS) was used to seed primary HUVEC cells at a density of 2 × 104 cells/well. The following day, fruquintinib was applied to the cells for eighteen hours at 37 degrees Celsius. The AlamarBlue assay was used to assess cell survival. After three hours of incubation at 37 C, the fluorescence value of the plates was measured on Tecan at Ex 530 nm and Em 590 nm.
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| Animal Protocol |
Mice: The xenograft models derived from patients are created subsequent to the primary tumor undergoing multiple in vivo passages. When tumors reach a size of 100–300 mm3, the animals are divided into groups of 6–8 at random. For three weeks, the mice are given either the vehicle (treated group) or a single daily dose of fruquintinib (0.5–20 mg/kg) suspended in the vehicle (control group). In combination studies, intravenous injections of either oxaliplatin (10 mg/kg) or docetaxel (Taxotere, 5 mg/kg) are given once a week to nude mice. Three times a week, body weight and tumor size are measured. TVs, or tumor volumes, are computed.
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| References |
| Molecular Formula |
C21H19N3O5
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| Molecular Weight |
393.39
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| Exact Mass |
393.13
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| Elemental Analysis |
C, 64.12; H, 4.87; N, 10.68; O, 20.34
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| CAS # |
1194506-26-7
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CC1=C(C2=C(O1)C=C(C=C2)OC3=NC=NC4=CC(=C(C=C43)OC)OC)C(=O)NC
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| InChi Key |
BALLNEJQLSTPIO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H19N3O5/c1-11-19(20(25)22-2)13-6-5-12(7-16(13)28-11)29-21-14-8-17(26-3)18(27-4)9-15(14)23-10-24-21/h5-10H,1-4H3,(H,22,25)
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| Chemical Name |
6-(6,7-dimethoxyquinazolin-4-yl)oxy-N,2-dimethyl-1-benzofuran-3-carboxamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.59 mg/mL (1.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.9 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.59 mg/mL (1.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.9 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.59 mg/mL (1.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5420 mL | 12.7100 mL | 25.4201 mL | |
| 5 mM | 0.5084 mL | 2.5420 mL | 5.0840 mL | |
| 10 mM | 0.2542 mL | 1.2710 mL | 2.5420 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05795296 | Active Recruiting |
Drug: Fruquintinib Drug: Sintilimab |
Stomach Neoplasms | RenJi Hospital | December 1, 2022 | Phase 2 |
| NCT04322539 | Active Recruiting |
Drug: Fruquintinib Drug: Placebo |
Metastatic Colorectal Cancer Metastatic Colon Cancer |
Hutchison Medipharma Limited | August 12, 2020 | Phase 3 |
| NCT03251378 | Active Recruiting |
Drug: Fruquintinib (HMPL-013) |
Rectal Cancer Advanced Solid Tumors |
Hutchmed | November 10, 2017 | Phase 1 |
| NCT06018714 | Recruiting | Drug: Fruquintinib | Colorectal Cancer Metastatic | Sun Yat-sen University | May 1, 2023 | Phase 2 |
| NCT05142631 | Recruiting | Drug: Fruquintinib | Soft Tissue Sarcoma | Fudan University | November 21, 2021 | Phase 2 |
Fruquintinib is a highly selective and potent VEGFR1, 2, 3 kinase inhibitor.Cancer Biol Ther.2014;15(12):1635-45. |
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Fruquintinib inhibited HUVEC tubule growth and CAM angiogenesis.Cancer Biol Ther.2014;15(12):1635-45. |
Combination of fruquintinib with chemo drugs shows enhanced anti-tumor effect in PDX models.Cancer Biol Ther.2014;15(12):1635-45. |
Inhibition on VEGF stimulated activation of KDR and VEGFR3.Cancer Biol Ther.2014;15(12):1635-45. |
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Fruquintinib inhibited BGC-823 and Caki-1 tumor growth and anti-angiogenesis in tumor tissues.Cancer Biol Ther.2014;15(12):1635-45. |
Fruquintinib inhibited p-KDR in lung tissues of mice. (A) Fruquintinib inhibited VEGF-A induced p-KDR in lung tissues. Each group was composed of 3 mice (m1, m2, m3). Animals were treated as described in Method section.Cancer Biol Ther.2014;15(12):1635-45. |
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