MedKoo Cat#: 145638 | Name: Rezivertinib

Description:

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

Rezivertinib (BPI-7711) is a novel third-generation EGFR tyrosine kinase inhibitor (TKI) targeting both EGFR-sensitizing mutations and EGFR T790M mutation. Rezivertinib is found to have promising efficacy and favorable safety profile for patients with locally advanced or metastatic/recurrent NSCLC with EGFR T790M mutation.

Chemical Structure

Rezivertinib
Rezivertinib
CAS#1835667-12-3

Theoretical Analysis

MedKoo Cat#: 145638

Name: Rezivertinib

CAS#: 1835667-12-3

Chemical Formula: C27H30N6O3

Exact Mass: 486.2400

Molecular Weight: 486.58

Elemental Analysis: C, 66.65; H, 6.21; N, 17.27; O, 9.86

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 #
No Data
Synonym
Rezivertinib;
IUPAC/Chemical Name
N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide
InChi Key
BPMZUKYFIDPLEA-UHFFFAOYSA-N
InChi Code
1S/C27H30N6O3/c1-6-26(34)29-22-15-21(24(35-5)16-25(22)36-14-13-32(2)3)31-27-28-12-11-20(30-27)19-17-33(4)23-10-8-7-9-18(19)23/h6-12,15-17H,1,13-14H2,2-5H3,(H,29,34)(H,28,30,31)
SMILES Code
COC1=C(NC2=NC(=CC=N2)C3=CN(C)C4=CC=CC=C34)C=C(NC(=O)C=C)C(OCCN(C)C)=C1
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

Preparing Stock Solutions

The following data is based on the product molecular weight 486.58 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: 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. 2: Shi Y, Wu S, Wang K, Cang S, Yao W, Fan Y, Wu L, Huang M, Li X, Pan Y, Yang Z, Zhu B, Chen G, Shi J, Sun M, Fang J, Wang L, Chen Z, Liu C, Li J, Liu J, Sun S, Zhao Y, Guo Y, Meng Z, Liu Z, Han Z, Lu H, Ma R, Hu S, Zhao G, Liu Z, Xie C, Zhong D, Zhao H, Yu H, Zhang L, Bi M, Yi S, Guo S, Yi T, Li W, Lin Y, Shu Y, Chen Z, Guo Z, Greco M, Wang T, Shen H. Efficacy and Safety of Rezivertinib (BPI-7711) in Patients With Locally Advanced or Metastatic/Recurrent EGFR T790M-Mutated NSCLC: A Phase 2b Study. J Thorac Oncol. 2022 Nov;17(11):1306-1317. doi: 10.1016/j.jtho.2022.08.015. Epub 2022 Aug 29. PMID: 36049654. 3: Yang S, Wu S, Zhao Y, Chen G, Zhu B, Li X, Wang K, Shi J, Cang S, Yao W, Fan Y, Fang J, Zhang L, Zhou J, Wu L, Zheng R, Huang M, Pan Y, Yang Z, Sun M, Yu H, Wang D, Huang J, Wang L, Shu Y, Chen Z, Liu C, Li J, Liu J, Sun S, Guo Y, Meng Z, Liu Z, Han Z, Wu G, Lu H, Ma R, Hu S, Zhao G, Zhang L, Liu Z, Xie C, Zhong D, Zhao H, Bi M, Yi S, Guo S, Yi T, Li W, Lin Y, Chen Z, Zhuang Z, Guo Z, Greco M, Wang T, Zhou A, Shi Y. Central nervous system efficacy of rezivertinib (BPI-7711) in advanced NSCLC patients with EGFR T790M mutation: A pooled analysis of two clinical studies. Lung Cancer. 2023 Jun;180:107194. doi: 10.1016/j.lungcan.2023.107194. Epub 2023 Apr 17. PMID: 37163774. 4: Shi Y, Zhou J, Zhao Y, Zhu B, Zhang L, Li X, Fang J, Shi J, Zhuang Z, Yang S, Wang D, Yu H, Zhang L, Zheng R, Greco M, Wang T. Results of the phase IIa study to evaluate the efficacy and safety of rezivertinib (BPI-7711) for the first- line treatment of locally advanced or metastatic/recurrent NSCLC patients with EGFR mutation from a phase I/IIa study. BMC Med. 2023 Jan 8;21(1):11. doi: 10.1186/s12916-022-02692-8. PMID: 36617560; PMCID: PMC9827694. 5: 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. 6: Shi Y, Zhao Y, Yang S, Zhou J, Zhang L, Chen G, Fang J, Zhu B, Li X, Shu Y, Shi J, Zheng R, Wang D, Yu H, Huang J, Zhuang Z, Wu G, Zhang L, Guo Z, Greco M, Li X, Zhang Y. Safety, Efficacy, and Pharmacokinetics of Rezivertinib (BPI-7711) in Patients With Advanced NSCLC With EGFR T790M Mutation: A Phase 1 Dose- Escalation and Dose-Expansion Study. J Thorac Oncol. 2022 May;17(5):708-717. doi: 10.1016/j.jtho.2022.01.015. Epub 2022 Feb 15. PMID: 35181498. 7: Medical Oncology Branch of China International Exchange and Promotive Association for Medical and Health Care; Chinese Association for Clinical Oncologists. [China clinical practice guideline for epidermal growth factor receptor tyrosine kinase inhibitors in stage Ⅳ non-small cell lung cancer (version 2023)]. Zhonghua Yi Xue Za Zhi. 2023 Oct 31;103(40):3160-3173. Chinese. doi: 10.3760/cma.j.cn112137-20230505-00725. PMID: 37879869. 8: Fukuda S, Suda K, Hamada A, Oiki H, Ohara S, Ito M, Soh J, Mitsudomi T, Tsutani Y. Potential Utility of a 4th-Generation EGFR-TKI and Exploration of Resistance Mechanisms-An In Vitro Study. Biomedicines. 2024 Jun 25;12(7):1412. doi: 10.3390/biomedicines12071412. PMID: 39061985; PMCID: PMC11273927.