| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Alflutinib mesylate (formerly also known as AST-2818; AST2818; Furmonertinib), the mesylate salt form of Alflutinib, is a novel, irreversible and 3rd generation EGFR (epidermal growth factor receptor) tyrosine kinase inhibitor (TKI) selective for EGFR T790M mutation. It inhibits the growth of tumors by targeting T790M and mutations that activate EGFR. On March 3, 2021, China approved alflutinib for the treatment of EGFR T790M+ non-small cell lung cancer. Alflutinib and gefitinib are being compared in the phase 3 trial FLAG for the first-line treatment of patients with EGFR+ NSCLC (NCT03787992).
| Targets |
CYP3A4 (EC50 = 0.25 μM); EGFR
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|---|---|
| ln Vitro |
Firmonertinib mesylate can suppress both the T790M acquired resistance mutation and EGFR active mutations[1].
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| References |
| Molecular Formula |
C29H35F3N8O5S
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|---|---|
| Molecular Weight |
664.699014902115
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| Exact Mass |
664.24
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| Elemental Analysis |
C, 52.40; H, 5.31; F, 8.57; N, 16.86; O, 12.03; S, 4.82
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| CAS # |
2130958-55-1
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| Related CAS # |
Firmonertinib;1869057-83-9
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| Appearance |
Solid powder
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| SMILES |
CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(N=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OCC(F)(F)F.CS(=O)(=O)O
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| InChi Key |
WDPGHXINXNBHAS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H31F3N8O2.CH4O3S/c1-6-24(40)33-21-15-22(26(41-17-28(29,30)31)36-25(21)38(4)14-13-37(2)3)35-27-32-12-11-20(34-27)19-16-39(5)23-10-8-7-9-18(19)23;1-5(2,3)4/h6-12,15-16H,1,13-14,17H2,2-5H3,(H,33,40)(H,32,34,35);1H3,(H,2,3,4)
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| Chemical Name |
N-[2-[2-(dimethylamino)ethyl-methylamino]-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]-6-(2,2,2-trifluoroethoxy)pyridin-3-yl]prop-2-enamide;methanesulfonic acid
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| Synonyms |
Furmonertinib; AST-2818; AST 2818 mesylate; AST2818 mesylate
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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 |
| 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) |
DMSO: 5~20 mg/mL (7.5~30.1 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (0.75 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 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 0.5 mg/mL (0.75 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 5.0 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: ≥ 0.5 mg/mL (0.75 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 | 1.5044 mL | 7.5222 mL | 15.0444 mL | |
| 5 mM | 0.3009 mL | 1.5044 mL | 3.0089 mL | |
| 10 mM | 0.1504 mL | 0.7522 mL | 1.5044 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 |
| NCT04858958 | Recruiting | Drug: Furmonertinib 160mg Drug: Furmonertinib 240mg |
NSCLC | Allist Pharmaceuticals, Inc. | August 10, 2020 | Phase 1 |
| NCT05987826 | Not yet recruiting | Drug: Furmonertinib | Non-Small Cell Lung Cancer | Shanghai Zhongshan Hospital | August 2023 | Phase 2 |
| NCT04965831 | Not yet recruiting | Drug: Furmonertinib | Lung Adenocarcinoma | Tianjin Medical University Cancer Institute and Hospital |
August 1, 2021 | Phase 2 |
| NCT05466149 | Recruiting | Drug: Furmonertinib | NSCLC | Allist Pharmaceuticals, Inc. | September 27, 2022 | Phase 2 |
| NCT05334277 | Recruiting | Drug: Furmonertinib/Pemetrexed /Carboplatin Drug: Furmonertinib |
Non-small Cell Lung Cancer | Sun Yat-sen University | May 6, 2022 | Phase 2 |
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