Abivertinib HCl

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MedKoo CAT#: 207122

CAS#: 1557268-90-2 (2HCl)

Description: Abivertinib, also known as AC0010 and Avitinib, is a third-generation EGFR tyrosine kinase inhibitor and BTK Inhibitor that demonstrated clinical efficacy and manageable adverse events (AEs). Abivertinib inhibits cell proliferation, reduces colony-forming capacity, and induces apoptosis and cell cycle arrest in AML cells, especially those harboring FLT3-ITD mutations. Abivertinib was also found to be more sensitive than ibrutinib in treating AML. Abivertinib may be a promising novel agent for AML, with potential for combination treatment with HHT.

Chemical Structure

Abivertinib HCl
CAS# 1557268-90-2 (2HCl)

Theoretical Analysis

MedKoo Cat#: 207122
Name: Abivertinib HCl
CAS#: 1557268-90-2 (2HCl)
Chemical Formula: C26H28Cl2FN7O2
Exact Mass:
Molecular Weight: 560.4554
Elemental Analysis: C, 55.72; H, 5.04; Cl, 12.65; F, 3.39; N, 17.49; O, 5.71

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Related CAS #: 1557267-42-1 (free base)   1557268-88-8 (maleate)   1822357-78-7 (maleate hydrate)   1557268-90-2 (2HCl)   1801879-16-2 (HCl)    

Synonym: Abivertinib maleate, Abivertinib; AC0010; AC-0010; AC 0010; Avitinib;

IUPAC/Chemical Name: N-(3-((2-((3-fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide dihydrochloride


InChi Code: InChI=1S/C26H26FN7O2.2ClH/c1-3-23(35)29-17-5-4-6-19(15-17)36-25-20-9-10-28-24(20)31-26(32-25)30-18-7-8-22(21(27)16-18)34-13-11-33(2)12-14-34;;/h3-10,15-16H,1,11-14H2,2H3,(H,29,35)(H2,28,30,31,32);2*1H

SMILES Code: C=CC(NC1=CC=CC(OC2=C3C(NC=C3)=NC(NC4=CC=C(N5CCN(C)CC5)C(F)=C4)=N2)=C1)=O.[H]Cl.[H]Cl

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

Preparing Stock Solutions

The following data is based on the product molecular weight 560.4554 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.

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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

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This message contains search results from the National Center for Biotechnology Information (NCBI) at the U.S. National Library of Medicine (NLM). Do not reply directly to this message

Sent On: Wed May 06 16:08:32 2020

12 selected items

PubMed Results
Items 1-12 of 12 (Display the 12 citations in PubMed)

1: Huang S, Yu M, Shi N, Zhou Y, Li F, Li X, Huang X, Jin J. Apigenin and Abivertinib, a novel BTK inhibitor synergize to inhibit diffuse large B-cell lymphoma in vivo and vitro. J Cancer. 2020 Feb 3;11(8):2123-2132. doi: 10.7150/jca.34981. PMID: 32127939; PMCID: PMC7052937.

2: Wang H, Pan R, Zhang X, Si X, Wang M, Zhang L. Abivertinib in patients with T790M-positive advanced NSCLC and its subsequent treatment with osimertinib. Thorac Cancer. 2020 Mar;11(3):594-602. doi: 10.1111/1759-7714.13302. Epub 2020 Jan 14. PMID: 31943845; PMCID: PMC7049520.

3: Zheng X, Wang W, Zhang Y, Ma Y, Zhao H, Gao H, Hu P, Jiang J. Development of an LC-MS/MS method for quantifying two main metabolites of abivertinib in human plasma. Biomed Chromatogr. 2020 Feb;34(2):e4704. doi: 10.1002/bmc.4704. Epub 2019 Dec 23. PMID: 31629371.

4: Yao X, Du N, Hu S, Wang L, Gao J. Rapid advances in research on and development of anticancer drugs in China. Biosci Trends. 2019 Nov 13;13(5):461-463. doi: 10.5582/bst.2019.01243. Epub 2019 Sep 10. PMID: 31511442.

5: Huang S, Pan J, Jin J, Li C, Li X, Huang J, Huang X, Yan X, Li F, Yu M, Hu C, Jin J, Xu Y, Ling Q, Ye W, Wang Y, Jin J. Abivertinib, a novel BTK inhibitor: Anti-Leukemia effects and synergistic efficacy with homoharringtonine in acute myeloid leukemia. Cancer Lett. 2019 Oct 1;461:132-143. doi: 10.1016/j.canlet.2019.07.008. Epub 2019 Jul 13. PMID: 31310800.

6: Zhang YC, Chen ZH, Zhang XC, Xu CR, Yan HH, Xie Z, Chuai SK, Ye JY, Han-Zhang H, Zhang Z, Bai XY, Su J, Gan B, Yang JJ, Li WF, Tang W, Luo FR, Xu X, Wu YL, Zhou Q. Analysis of resistance mechanisms to abivertinib, a third-generation EGFR tyrosine kinase inhibitor, in patients with EGFR T790M-positive non-small cell lung cancer from a phase I trial. EBioMedicine. 2019 May;43:180-187. doi: 10.1016/j.ebiom.2019.04.030. Epub 2019 Apr 23. PMID: 31027916; PMCID: PMC6558024.

7: Roskoski R Jr. Small molecule inhibitors targeting the EGFR/ErbB family of protein-tyrosine kinases in human cancers. Pharmacol Res. 2019 Jan;139:395-411. doi: 10.1016/j.phrs.2018.11.014. Epub 2018 Nov 27. PMID: 30500458.

8: Attwa MW, Kadi AA, Abdelhameed AS. Reactive intermediates and bioactivation pathways characterization of avitinib by LC-MS/MS: In vitro metabolic investigation. J Pharm Biomed Anal. 2019 Feb 5;164:659-667. doi: 10.1016/j.jpba.2018.11.033. Epub 2018 Nov 17. PMID: 30472584.

9: Wang H, Zhang L, Hu P, Zheng X, Si X, Zhang X, Wang M. Penetration of the blood-brain barrier by avitinib and its control of intra/extra-cranial disease in non-small cell lung cancer harboring the T790M mutation. Lung Cancer. 2018 Aug;122:1-6. doi: 10.1016/j.lungcan.2018.05.010. Epub 2018 May 21. PMID: 30032814.

10: Ma Y, Zheng X, Zhao H, Fang W, Zhang Y, Ge J, Wang L, Wang W, Jiang J, Chuai S, Zhang Z, Xu W, Xu X, Hu P, Zhang L. First-in-Human Phase I Study of AC0010, a Mutant-Selective EGFR Inhibitor in Non-Small Cell Lung Cancer: Safety, Efficacy, and Potential Mechanism of Resistance. J Thorac Oncol. 2018 Jul;13(7):968-977. doi: 10.1016/j.jtho.2018.03.025. Epub 2018 Apr 4. PMID: 29626621.

11: Wang W, Zheng X, Wang H, Wang L, Jiang J, Hu P. Development of an UPLC-MS/MS method for quantification of Avitinib (AC0010) and its five metabolites in human cerebrospinal fluid: Application to a study of the blood-brain barrier penetration rate of non-small cell lung cancer patients. J Pharm Biomed Anal. 2017 May 30;139:205-214. doi: 10.1016/j.jpba.2017.02.057. Epub 2017 Mar 4. PMID: 28285073.

12: Xu X. Parallel phase 1 clinical trials in the US and in China: accelerating the test of avitinib in lung cancer as a novel inhibitor selectively targeting mutated EGFR and overcoming T790M-induced resistance. Chin J Cancer. 2015 Jul 8;34(7):285-7. doi: 10.1186/s40880-015-0029-3. PMID: 26152224; PMCID: PMC4593347.

Additional Information

Resistance to third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) presents a major clinical challenge in advanced non-small cell lung cancer (NSCLC).