MedKoo Cat#: 535184 | Name: Befotertinib
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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
Befotertinib
CAS#1835667-63-4 (free base)

Theoretical Analysis

MedKoo Cat#: 535184

Name: Befotertinib

CAS#: 1835667-63-4 (free base)

Chemical Formula: C29H32F3N7O2

Exact Mass: 567.2570

Molecular Weight: 567.62

Elemental Analysis: C, 61.37; H, 5.68; F, 10.04; N, 17.27; O, 5.64

Price and Availability

Size Price Availability Quantity
5mg USD 650.00 2 Weeks
10mg USD 1,150.00 2 Weeks
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Synonym
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]prop-2-enamide
InChi Key
USOCZVZOXKTJTI-UHFFFAOYSA-N
InChi Code
InChI=1S/C29H32F3N7O2/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/h6-12,15-17H,1,13-14,18H2,2-5H3,(H,34,40)(H,33,35,36)
SMILES Code
C=CC(NC1=CC(NC2=NC=CC(C3=CN(CC(F)(F)F)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=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

Preparing Stock Solutions

The following data is based on the product molecular weight 567.62 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: 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.