Befotertinib | EGFR | tyrosine kinase inhibitor | antineoplastic

MedKoo Cat#: 124655 | Name: Befotertinib mesylate

Description:

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

Befotertinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, antineoplastic.

Chemical Structure

Befotertinib mesylate

CAS#2226167-02-6 (mesylate)

Theoretical Analysis

MedKoo Cat#: 124655

Name: Befotertinib mesylate

CAS#: 2226167-02-6 (mesylate)

Chemical Formula: C30H36F3N7O5S

Exact Mass: 0.0000

Molecular Weight: 663.72

Elemental Analysis: C, 54.29; H, 5.47; F, 8.59; N, 14.77; O, 12.05; S, 4.83

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 #

1835667-63-4 (free base) 2226167-02-6 (mesylate)

Synonym

Befotertinib mesylate; Befotertinib monomesilate; Befotertinib monomesylate; Befotertinib; D-0316; D 0316; D0316;

IUPAC/Chemical Name

N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-(2,2,2-trifluoroethyl)-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide methanesulfonate

InChi Key

FFQDXZLQXPZZDJ-UHFFFAOYSA-N

InChi Code

InChI=1S/C29H32F3N7O2.CH4O3S/c1-6-27(40)34-22-15-23(26(41-5)16-25(22)38(4)14-13-37(2)3)36-28-33-12-11-21(35-28)20-17-39(18-29(30,31)32)24-10-8-7-9-19(20)24;1-5(2,3)4/h6-12,15-17H,1,13-14,18H2,2-5H3,(H,34,40)(H,33,35,36);1H3,(H,2,3,4)

SMILES Code

CN(C)CCN(C)C1=CC(=C(C=C1NC(=O)C=C)NC2=NC=CC(=N2)C3=CN(C4=CC=CC=C43)CC(F)(F)F)OC.CS(=O)(=O)O

Appearance

To be determined

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

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

To be determined

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 663.72 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: Blair HA. Befotertinib: First Approval. Drugs. 2023 Oct;83(15):1433-1437. doi: 10.1007/s40265-023-01946-w. PMID: 37751131. 2: Lu S, Zhou J, Jian H, Wu L, Cheng Y, Fan Y, Fang J, Chen G, Zhang Z, Lv D, Jiang L, Wu R, Jin X, Zhang X, Zhang J, Xie C, Sun G, Huang D, Cui J, Guo R, Han Z, Chen Z, Liang J, Zhuang W, Hu X, Zang A, Zhang Y, Cang S, Lan Y, Chen X, Liu L, Li X, Chen J, Ma R, Guo Y, Sun P, Tian P, Pan Y, Liu Z, Cao P, Ding L, Wang Y, Yuan X, Wu P. Befotertinib (D-0316) versus icotinib as first-line therapy for patients with EGFR-mutated locally advanced or metastatic non-small-cell lung cancer: a multicentre, open-label, randomised phase 3 study. Lancet Respir Med. 2023 Oct;11(10):905-915. doi: 10.1016/S2213-2600(23)00183-2. Epub 2023 May 24. PMID: 37244266. 3: Lu S, Zhang Y, Zhang G, Zhou J, Cang S, Cheng Y, Wu G, Cao P, Lv D, Jian H, Chen C, Jin X, Tian P, Wang K, Jiang G, Chen G, Chen Q, Zhao H, Ding C, Guo R, Sun G, Wang B, Jiang L, Liu Z, Fang J, Yang J, Zhuang W, Liu Y, Zhang J, Pan Y, Chen J, Yu Q, Zhao M, Cui J, Li D, Yi T, Yu Z, Yang Y, Zhang Y, Zhi X, Huang Y, Wu R, Chen L, Zang A, Cao L, Li Q, Li X, Song Y, Wang D, Zhang S, Ding L, Zhang L, Yuan X, Yao L, Shen Z. Efficacy and Safety of Befotertinib (D-0316) in Patients With EGFR T790M-Mutated NSCLC That Had Progressed After Prior EGFR Tyrosine Kinase Inhibitor Therapy: A Phase 2, Multicenter, Single-Arm, Open- Label Study. J Thorac Oncol. 2022 Oct;17(10):1192-1204. doi: 10.1016/j.jtho.2022.06.002. Epub 2022 Jun 18. PMID: 35724798. 4: Lu S, Zhang Y, Zhang G, Zhou J, Cang S, Cheng Y, Wu G, Cao P, Lv D, Jian H, Jin X, Chen C, Tian P, Wang K, Jiang G, Chen G, Chen Q, Zhao H, Ding C, Guo R, Sun G, Wang B, Jiang L, Liu Z, Fang J, Yang J, Zhuang W, Liu Y, Zhang J, Pan Y, Chen J, Yu Q, Zhao M, Cui J, Li D, Yi T, Yu Z, Yang Y, Zhang Y, Zhi X, Huang Y, Wu R, Chen L, Zang A, Cao L, Li Q, Li X, Song Y, Wang D, Zhang S, Ding L, Zhang L, Ji D, Shen Z. Befotertinib for patients with pretreated EGFR T790M mutated locally advanced or metastatic NSCLC: Final overall survival results from a phase 2 trial. Lung Cancer. 2024 Sep;195:107901. doi: 10.1016/j.lungcan.2024.107901. Epub 2024 Jul 27. PMID: 39089004. 5: 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. 6: Menis J, Remon J. Befotertinib-a viable alternative in EGFR-mutant advanced NSCLC? Lancet Respir Med. 2023 Oct;11(10):857-859. doi: 10.1016/S2213-2600(23)00216-3. Epub 2023 May 24. PMID: 37244264. 7: Sacchi de Camargo Correia G, Lou Y, Manochakian R. Befotertinib: one more drug targeting EGFR-the more may be the merrier. Chin Clin Oncol. 2024 Aug 13:cco-24-50. doi: 10.21037/cco-24-50. Epub ahead of print. PMID: 39168634. 8: Zhang Z, Huang Y, Gu H, Zhao L, Zhao B. Efficacy of befotertinib in non-small cell lung cancer harboring uncommon compound EGFR mutations G719X and S768I: a case report. Front Oncol. 2024 Apr 4;14:1370666. doi: 10.3389/fonc.2024.1370666. PMID: 38638860; PMCID: PMC11024360. 9: Li H, Wang Y, Ding R, Chen C, Tian Z, Yin H, Ding L. Simultaneous quantitation of befotertinib (D-0316) and its metabolite D-0865 in human plasma by LC-MS/MS method. J Chromatogr B Analyt Technol Biomed Life Sci. 2023 Jan 1;1214:123499. doi: 10.1016/j.jchromb.2022.123499. Epub 2022 Oct 17. PMID: 36525886. 10: Sørensen JB, Santoni-Rugiu E, Urbanska EM. Befotertinib in first-line treatment for Chinese non-small cell lung cancer patients harboring common EGFR- mutations reveals similar efficacy to other third-generation EGFR-TKIs but somewhat different safety profile. Chin Clin Oncol. 2024 Aug 22:cco-24-19. doi: 10.21037/cco-24-19. Epub ahead of print. PMID: 39260433.