Alflutinib mesylate | CAS# 2130958-55-1 | EGFR Inhibitor

MedKoo Cat#: 573651 | Name: Alflutinib mesylate

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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 mesylate

CAS#2130958-55-1 (mesylate)

Theoretical Analysis

MedKoo Cat#: 573651

Name: Alflutinib mesylate

CAS#: 2130958-55-1 (mesylate)

Chemical Formula: C29H35F3N8O5S

Exact Mass: 664.2403

Molecular Weight: 664.70

Elemental Analysis: C, 52.40; H, 5.31; F, 8.57; N, 16.86; O, 12.03; S, 4.82

Price and Availability

Size	Price	Availability
10mg	USD 350.00	2 Weeks
25mg	USD 650.00	2 Weeks
50mg	USD 950.00	2 Weeks

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Related CAS #

2130958-55-1 (mesylate) 1869057-83-9 (free base)

Synonym

Alflutinib mesylate, AST-2818 mesylate, AST2818; AST-2818; AST 2818; Furmonertinib;

IUPAC/Chemical Name

N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)-6-(2,2,2-trifluoroethoxy)pyridin-3-yl)acrylamide methanesulfonate

InChi Key

WDPGHXINXNBHAS-UHFFFAOYSA-N

InChi Code

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)

SMILES Code

CN(C)CCN(C)c1nc(OCC(F)(F)F)c(Nc2nccc(n2)c3cn(C)c4ccccc34)cc1NC(=O)C=C.CS(=O)(=O)O

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 664.70 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.

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: 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. 2: Deeks ED. Furmonertinib: First Approval. Drugs. 2021 Oct;81(15):1775-1780. doi: 10.1007/s40265-021-01588-w. PMID: 34528187. 3: 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. 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 Nov;17(11):1297-1305. doi: 10.1016/j.jtho.2022.07.1143. Epub 2022 Aug 3. PMID: 35932953. 5: 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. 6: 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. 7: 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. 8: Nagasaka M, Zhu VW, Lim SM, Greco M, Wu F, Ou SI. Beyond Osimertinib: The Development of Third-Generation EGFR Tyrosine Kinase Inhibitors For Advanced EGFR+ NSCLC. J Thorac Oncol. 2021 May;16(5):740-763. doi: 10.1016/j.jtho.2020.11.028. Epub 2020 Dec 15. PMID: 33338652. 9: Lau SCM, Ou SI. And Still They Come Over Troubled Waters: Can Asia's Third- Generation EGFR Tyrosine Kinase Inhibitors (Furmonertinib, Aumolertinib, Rezivertinib, Limertinib, Befotertinib, SH-1028, and Lazertinib) Affect Global Treatment of EGFR+ NSCLC. J Thorac Oncol. 2022 Oct;17(10):1144-1154. doi: 10.1016/j.jtho.2022.08.016. PMID: 36192074. 10: 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. 11: 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. 12: Li Y, Meng L, Ma Y, Li Y, Xing X, Guo C, Dong Z. Determination of Osimertinib, Aumolertinib, and Furmonertinib in Human Plasma for Therapeutic Drug Monitoring by UPLC-MS/MS. Molecules. 2022 Jul 13;27(14):4474. doi: 10.3390/molecules27144474. PMID: 35889345; PMCID: PMC9325192. 13: 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. 14: 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. 15: Jiang W, Sha M, Chen C. Successful Salvage Therapy With a High Dose of Furmonertinib in a Case of Lung Adenocarcinoma Harboring EGFR Exon 20 Insertion. Am J Ther. 2022 Apr 28. doi: 10.1097/MJT.0000000000001504. Epub ahead of print. PMID: 35482932. 16: Hu X, Zhang S, Ma Z, Feng J, Wu L, Lv D, Zhou J, Zhang X, Liu L, Yu Q, Liao W, Zhang Y, Wang X, Cheng Y, Niu H, Wang Z, Wang D, Huang C, Liu C, Zhao H, Feng J, Li J, Ying K, Yang N, Qin S, Hu J, Liu F, Jiang Y, Ge N, Shi Y. Central nervous system efficacy of furmonertinib (AST2818) in patients with EGFR T790M mutated non-small cell lung cancer: a pooled analysis from two phase 2 studies. BMC Med. 2023 Apr 28;21(1):164. doi: 10.1186/s12916-023-02865-z. PMID: 37118803; PMCID: PMC10148399. 17: Xu Z, Hao X, Wang Q, Yang K, Li J, Xing P. Intracranial efficacy and safety of furmonertinib 160 mg with or without anti-angiogenic agent in advanced NSCLC patients with BM/LM as salvage therapy. BMC Cancer. 2023 Mar 4;23(1):206. doi: 10.1186/s12885-023-10676-x. PMID: 36870951; PMCID: PMC9985196. 18: Zhang X, Han H, Zhao J, Liu X, Zhang J, Sun R, Li S, Liu B, Zhu H, Jiao S, Li X, Tang H. Case Report: A good response to furmonertinib second-line treatment of an advanced lung adenocarcinoma patient with a rare EGFR exon 20 N771_P772insH mutation: A case report and literature review. Front Pharmacol. 2022 Aug 17;13:964606. doi: 10.3389/fphar.2022.964606. PMID: 36059942; PMCID: PMC9432720. 19: Jia K, Yang S, Chen B, Yu J, Wu Y, Li W, Zhou F, Wu F, Feng G, Ren S. Advanced lung adenocarcinoma patient with EGFR exon 20 insertion benefits from high-dose furmonertinib for nine months after progression from mobocertinib: a case report. Ann Transl Med. 2022 Mar;10(6):386. doi: 10.21037/atm-22-1167. PMID: 35433998; PMCID: PMC9011291. 20: Chen X, Zha W, Su M, Meng N, Cao S, Niu B, Qi X. Persistent response of furmonertinib plus anlotinib in a lung adenocarcinoma patient with an EGFR exon 20 insertion mutation: A case report. Front Pharmacol. 2023 Feb 3;14:1053805. doi: 10.3389/fphar.2023.1053805. PMID: 36817153; PMCID: PMC9935568.

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MedKoo CAT#: 125708

CAS#: 17239-49-5