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MedKoo Cat#: 573650 | Name: Alflutinib

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Alflutinib, also known as AST 2818; Furmonertinib, is an EGFR inhibitor that targets both EGFR activating mutations and T790M, thus leading to tumor growth inhibition. Furmonertinibc has an advanced efficacy and a relatively wide safety window, has been commercially launched in China for the treatment of lung cancer patients with T790M-resistant mutations. It is metabolized mainly by the CYP3A4 enzyme.

Chemical Structure

Alflutinib
CAS#1869057-83-9 (free base)

Theoretical Analysis

MedKoo Cat#: 573650

Name: Alflutinib

CAS#: 1869057-83-9 (free base)

Chemical Formula: C28H31F3N8O2

Exact Mass: 568.2522

Molecular Weight: 568.61

Elemental Analysis: C, 59.15; H, 5.50; F, 10.02; N, 19.71; O, 5.63

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
2130958-55-1 (mesylate) 1869057-83-9 (free base)
Synonym
Alflutinib; AST-2818; AST2818; AST 2818; Furmonertinib; Firmonertinib
IUPAC/Chemical Name
2-Propenamide, N-(2-((2-(dimethylamino)ethyl)methylamino)-5-((4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl)amino)-6-(2,2,2-trifluoroethoxy)-3-pyridinyl)-
InChi Key
GHKOONMJXNWOIW-UHFFFAOYSA-N
InChi Code
1S/C28H31F3N8O2/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/h6-12,15-16H,1,13-14,17H2,2-5H3,(H,33,40)(H,32,34,35)
SMILES Code
CN(C)CCN(C)c1nc(OCC(F)(F)F)c(Nc2nccc(n2)c3cn(C)c4ccccc34)cc1NC(=O)C=C
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 568.61 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Wu Y, Chen L, Chen J, Xue H, He Q, Zhong D, Diao X. Covalent Binding Mechanism of Furmonertinib and Osimertinib With Human Serum Albumin. Drug Metab Dispos. 2023 Jan;51(1):8-16. doi: 10.1124/dmd.122.001019. Epub 2022 Nov 3. PMID: 36328480. 2: Zhang SS, Ou SI. Spotlight on Furmonertinib (Alflutinib, AST2818). The Swiss Army Knife (del19, L858R, T790M, Exon 20 Insertions, "uncommon-G719X, S768I, L861Q") Among the Third-Generation EGFR TKIs? Lung Cancer (Auckl). 2022 Oct 25;13:67-73. doi: 10.2147/LCTT.S385437. PMID: 36317157; PMCID: PMC9617553. 3: Cheng D, Tang S, Li D, Zhao W, Wei W, Fang C, Ji M. Successful salvage therapy using high-dose furmonertinib (AST2818) for non-small-cell lung cancer after Osimertinib resistance: a case report. Anticancer Drugs. 2022 Sep 1;33(8):768-772. doi: 10.1097/CAD.0000000000001368. Epub 2022 Aug 10. PMID: 35946524; PMCID: PMC9374065. 4: Shi Y, Chen G, Wang X, Liu Y, Wu L, Hao Y, Liu C, Zhu S, Zhang X, Li Y, Liu J, Cao L, Cheng Y, Zhao H, Zhang S, Zang A, Cui J, Feng J, Yang N, Liu F, Jiang Y, Gu C. Central Nervous System Efficacy of Furmonertinib (AST2818) Versus Gefitinib as First-Line Treatment for EGFR-Mutated NSCLC: Results From the FURLONG Study. J Thorac Oncol. 2022 Aug 3:S1556-0864(22)01496-4. doi: 10.1016/j.jtho.2022.07.1143. Epub ahead of print. PMID: 35932953. 5: Shi Y, Chen G, Wang X, Liu Y, Wu L, Hao Y, Liu C, Zhu S, Zhang X, Li Y, Liu J, Cao L, Cheng Y, Zhao H, Zhang S, Zang A, Cui J, Feng J, Yang N, Liu F, Jiang Y, Gu C; FURLONG investigators. Furmonertinib (AST2818) versus gefitinib as first-line therapy for Chinese patients with locally advanced or metastatic EGFR mutation-positive non-small-cell lung cancer (FURLONG): a multicentre, double- blind, randomised phase 3 study. Lancet Respir Med. 2022 Nov;10(11):1019-1028. doi: 10.1016/S2213-2600(22)00168-0. Epub 2022 Jun 2. PMID: 35662408. 6: Chen L, Zhou Y, Gan C, Wang X, Liu Y, Dong C, He R, Yang J. Three Third- Generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Non- Small Cell Lung Cancer: Similarities and Differences. Cancer Invest. 2022 Aug;40(7):590-603. doi: 10.1080/07357907.2022.2069254. Epub 2022 Apr 26. PMID: 35445633. 7: Heng J, Tang Q, Chen X, Bao J, Deng J, Chen Y, Zhao J, Zhu S, Liu X, Yang F, Jiang Y, Yang N, Li K. Corrigendum to ' Evaluation of the pharmacokinetic effects of itraconazole on alflutinib (AST2818): an open-label, single-center, single-sequence, two-period randomized study in healthy volunteers'[European Journal of Pharmaceutical Sciences 162 (2021) 105815]. Eur J Pharm Sci. 2022 Apr 1;171:106143. doi: 10.1016/j.ejps.2022.106143. Epub 2022 Feb 16. Erratum for: Eur J Pharm Sci. 2021 Jul 1;162:105815. PMID: 35181200. 8: Zou HX, Zhang YF, Zhong DF, Jiang Y, Liu F, Zhao QY, Zuo Z, Zhang YF, Yan XY. Effect of autoinduction and food on the pharmacokinetics of furmonertinib and its active metabolite characterized by a population pharmacokinetic model. Acta Pharmacol Sin. 2022 Jul;43(7):1865-1874. doi: 10.1038/s41401-021-00798-y. Epub 2021 Nov 17. PMID: 34789919; PMCID: PMC9252999. 9: Deeks ED. Furmonertinib: First Approval. Drugs. 2021 Oct;81(15):1775-1780. doi: 10.1007/s40265-021-01588-w. PMID: 34528187. 10: Wu YL, Xue YR, Guo ZT, Chen ZD, Ge XY, Zhong DF, Diao XX. Furmonertinib (Alflutinib, AST2818) is a potential positive control drug comparable to rifampin for evaluation of CYP3A4 induction in sandwich-cultured primary human hepatocytes. Acta Pharmacol Sin. 2022 Mar;43(3):747-756. doi: 10.1038/s41401-021-00692-7. Epub 2021 May 25. PMID: 34035488; PMCID: PMC8888569. 11: Meng J, Zhang H, Bao JJ, Chen ZD, Liu XY, Zhang YF, Jiang Y, Miao LY, Zhong DF. Metabolic disposition of the EGFR covalent inhibitor furmonertinib in humans. Acta Pharmacol Sin. 2022 Feb;43(2):494-503. doi: 10.1038/s41401-021-00667-8. Epub 2021 Apr 29. PMID: 33927359; PMCID: PMC8791928. 12: Shi Y, Hu X, Zhang S, Lv D, Wu L, Yu Q, Zhang Y, Liu L, Wang X, Cheng Y, Ma Z, Niu H, Wang D, Feng J, Huang C, Liu C, Zhao H, Li J, Zhang X, Jiang Y, Gu C. Efficacy, safety, and genetic analysis of furmonertinib (AST2818) in patients with EGFR T790M mutated non-small-cell lung cancer: a phase 2b, multicentre, single-arm, open-label study. Lancet Respir Med. 2021 Aug;9(8):829-839. doi: 10.1016/S2213-2600(20)30455-0. Epub 2021 Mar 26. PMID: 33780662. 13: Heng J, Tang Q, Chen X, Bao J, Deng J, Chen Y, Zhao J, Zhu S, Liu X, Yang F, Jiang Y, Yang N, Li K. Evaluation of the pharmacokinetic effects of itraconazole on alflutinib (AST2818): an open-label, single-center, single-sequence, two- period randomized study in healthy volunteers. Eur J Pharm Sci. 2021 Jul 1;162:105815. doi: 10.1016/j.ejps.2021.105815. Epub 2021 Mar 23. Erratum in: Eur J Pharm Sci. 2022 Apr 1;171:106143. PMID: 33771716. 14: Zhu S, Deng J, Tang Q, Heng J, Qu J, Chen Y, Chen X, Yang N, Liu X, Li K. A Randomized, Open, Single-Centre, Crossed Study of the Effect of Food on the Pharmacokinetics of One Oral Dose of Alflutinib Mesylate Tablets (AST2818) in Healthy Male Subjects. Iran J Pharm Res. 2020 Summer;19(3):24-33. doi: 10.22037/ijpr.2020.113112.14116. PMID: 33680007; PMCID: PMC7757978. 15: Zhu YT, Zhang YF, Jiang JF, Yang Y, Guo LX, Bao JJ, Zhong DF. Effects of rifampicin on the pharmacokinetics of alflutinib, a selective third-generation EGFR kinase inhibitor, and its metabolite AST5902 in healthy volunteers. Invest New Drugs. 2021 Aug;39(4):1011-1018. doi: 10.1007/s10637-021-01071-z. Epub 2021 Jan 27. PMID: 33506323. 16: Liu X, Feng D, Zheng M, Cui Y, Zhong D. Characterization of covalent binding of tyrosine kinase inhibitors to plasma proteins. Drug Metab Pharmacokinet. 2020 Oct;35(5):456-465. doi: 10.1016/j.dmpk.2020.07.002. Epub 2020 Jul 24. PMID: 32847720. 17: Liu XY, Guo ZT, Chen ZD, Zhang YF, Zhou JL, Jiang Y, Zhao QY, Diao XX, Zhong DF. Alflutinib (AST2818), primarily metabolized by CYP3A4, is a potent CYP3A4 inducer. Acta Pharmacol Sin. 2020 Oct;41(10):1366-1376. doi: 10.1038/s41401-020-0389-3. Epub 2020 Mar 31. PMID: 32235864; PMCID: PMC7608132. 18: Shi Y, Zhang S, Hu X, Feng J, Ma Z, Zhou J, Yang N, Wu L, Liao W, Zhong D, Han X, Wang Z, Zhang X, Qin S, Ying K, Feng J, Fang J, Liu L, Jiang Y. Safety, Clinical Activity, and Pharmacokinetics of Alflutinib (AST2818) in Patients With Advanced NSCLC With EGFR T790M Mutation. J Thorac Oncol. 2020 Jun;15(6):1015-1026. doi: 10.1016/j.jtho.2020.01.010. Epub 2020 Jan 30. Erratum in: J Thorac Oncol. 2020 Oct 16;: PMID: 32007598. 19: Liu X, Li W, Zhang Y, Jiang Y, Zhao Q, Zhong D. Simultaneous determination of alflutinib and its active metabolite in human plasma using liquid chromatography-tandem mass spectrometry. J Pharm Biomed Anal. 2019 Nov 30;176:112735. doi: 10.1016/j.jpba.2019.06.032. Epub 2019 Jul 16. PMID: 31394305.