Dacomitinib
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MedKoo CAT#: 205576

CAS#: 1110813-31-4 (free)

Description: Dacomitinib, also known as PF-299 and PF-00299804 ; or PF299804, is an orally bioavailable, highly selective, second-generation small-molecule inhibitor of the pan-epidermal growth factor receptor (EGFR) family of tyrosine kinases (ErbB family) with potential antineoplastic activity. Dacomitinib specifically and irreversibly binds to and inhibits human EGFR subtypes, resulting in inhibition of proliferation and induction of apoptosis in EGFR-expressing tumor cells. EGFRs play major roles in tumor cell proliferation and tumor vascularization, and are often overexpressed or mutated in various tumor cell types.


Price and Availability

Size Price Shipping out time Quantity
50mg USD 150 Same day
200mg USD 450 Same day
500mg USD 550 Same day
1g USD 950 Same day
2g USD 1650 Same day
5g USD 3650 Same day
10g USD 6550 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-08-11. Prices are subject to change without notice.

Dacomitinib (PF299804), purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 7g may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205576
Name: Dacomitinib
CAS#: 1110813-31-4 (free)
Chemical Formula: C24H25ClFN5O2
Exact Mass: 469.16808
Molecular Weight: 469.94
Elemental Analysis: C, 61.34; H, 5.36; Cl, 7.54; F, 4.04; N, 14.90; O, 6.81


Related CAS #: 1110813-31-4 (free)   1042385-75-0 (hydrate)   1262034-38-7    

Synonym: PF-00299804; PF00299804; PF 00299804; PF299804; PF-299804; PF 299804; PF-299; PF299; PF 299; Dacomitinib; Vizimpro;

IUPAC/Chemical Name: (E)-N-(4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)-4-(piperidin-1-yl)but-2-enamide

InChi Key: LVXJQMNHJWSHET-AATRIKPKSA-N

InChi Code: InChI=1S/C24H25ClFN5O2/c1-33-22-14-20-17(24(28-15-27-20)29-16-7-8-19(26)18(25)12-16)13-21(22)30-23(32)6-5-11-31-9-3-2-4-10-31/h5-8,12-15H,2-4,9-11H2,1H3,(H,30,32)(H,27,28,29)/b6-5+

SMILES Code: O=C(NC1=CC2=C(NC3=CC=C(F)C(Cl)=C3)N=CN=C2C=C1OC)/C=C/CN4CCCCC4


Technical Data

Appearance:
White to off-white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Safety Data Sheet (SDS):

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, not in water

Shelf Life:
>2 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


Additional Information

  
   
 


References

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2: Lavacchi D, Mazzoni F, Giaccone G. Clinical evaluation of dacomitinib for the treatment of metastatic non-small cell lung cancer (NSCLC): current perspectives. Drug Des Devel Ther. 2019 Sep 6;13:3187-3198. doi: 10.2147/DDDT.S194231. eCollection 2019. PubMed PMID: 31564835; PubMed Central PMCID: PMC6735534.

3: Iwasaku M, Uchino J, Yamada T, Chihara Y, Shimamoto T, Tamiya N, Kaneko Y, Kiyomi F, Takayama K. Rationale and design of a phase II study to evaluate prophylactic treatment of dacomitinib-induced dermatologic adverse events in epidermal growth factor receptor-mutated advanced non-small cell lung cancer (SPIRAL-Daco study). Transl Lung Cancer Res. 2019 Aug;8(4):519-523. doi: 10.21037/tlcr.2019.08.03. PubMed PMID: 31555524; PubMed Central PMCID: PMC6749124.

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5: Santarpia M, Menis J, Chaib I, Gonzalez Cao M, Rosell R. Dacomitinib for the first-line treatment of patients with EGFR-mutated metastatic non-small cell lung cancer. Expert Rev Clin Pharmacol. 2019 Sep;12(9):831-840. doi: 10.1080/17512433.2019.1649136. Epub 2019 Aug 5. Review. PubMed PMID: 31356117.

6: Corral J, Mok TS, Nakagawa K, Rosell R, Lee KH, Migliorino MR, Pluzanski A, Linke R, Devgan G, Tan W, Quinn S, Wang T, Wu YL. Effects of dose modifications on the safety and efficacy of dacomitinib for EGFR mutation-positive non-small-cell lung cancer. Future Oncol. 2019 Aug;15(24):2795-2805. doi: 10.2217/fon-2019-0299. Epub 2019 Jul 17. PubMed PMID: 31313942.

7: Jathal MK, Steele TM, Siddiqui S, Mooso BA, D'Abronzo LS, Drake CM, Whang YE, Ghosh PM. Dacomitinib, but not lapatinib, suppressed progression in castration-resistant prostate cancer models by preventing HER2 increase. Br J Cancer. 2019 Jul;121(3):237-248. doi: 10.1038/s41416-019-0496-4. Epub 2019 Jun 18. PubMed PMID: 31209328; PubMed Central PMCID: PMC6738116.

8: Lau SCM, Batra U, Mok TSK, Loong HH. Dacomitinib in the Management of Advanced Non-Small-Cell Lung Cancer. Drugs. 2019 Jun;79(8):823-831. doi: 10.1007/s40265-019-01115-y. Review. PubMed PMID: 31069718.

9: Nagano T, Tachihara M, Nishimura Y. Dacomitinib, a second-generation irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) to treat non-small cell lung cancer. Drugs Today (Barc). 2019 Apr;55(4):231-236. doi: 10.1358/dot.2019.55.4.2965337. Review. PubMed PMID: 31050691.

10: Momeny M, Esmaeili F, Hamzehlou S, Yousefi H, Javadikooshesh S, Vahdatirad V, Alishahi Z, Mousavipak SH, Bashash D, Dehpour AR, Tavangar SM, Tavakkoly-Bazzaz J, Haddad P, Kordbacheh F, Alimoghaddam K, Ghavamzadeh A, Ghaffari SH. The ERBB receptor inhibitor dacomitinib suppresses proliferation and invasion of pancreatic ductal adenocarcinoma cells. Cell Oncol (Dordr). 2019 Aug;42(4):491-504. doi: 10.1007/s13402-019-00448-w. Epub 2019 Apr 25. PubMed PMID: 31025257.

11: Abdelhameed AS, Kadi AA, Attwa MW, AlRabiah H. Validated LC-MS/MS assay for quantification of the newly approved tyrosine kinase inhibitor, dacomitinib, and application to investigating its metabolic stability. PLoS One. 2019 Apr 4;14(4):e0214598. doi: 10.1371/journal.pone.0214598. eCollection 2019. PubMed PMID: 30947315; PubMed Central PMCID: PMC6448865.

12: Zhou Q, Wu YL, Corral J, Nakagawa K, Garon EB, Sbar EI, Wang T, Sandin R, Noonan K, Gernhardt D, Mok TS. Management of common adverse events related to first-line dacomitinib use in EGFR mutation-positive non-small-cell lung cancer: a pooled safety analysis. Future Oncol. 2019 May;15(13):1481-1491. doi: 10.2217/fon-2018-0944. Epub 2019 Mar 6. PubMed PMID: 30839234.

13: Chen WS, Hong L, Wang F, Li JJ. Investigation of dacomitinib on reducing cell necrosis and enhancing cell apoptosis in C6 glioma rat model by MRI. Biosci Rep. 2019 Mar 6;39(3). pii: BSR20190006. doi: 10.1042/BSR20190006. Print 2019 Mar 29. PubMed PMID: 30782784; PubMed Central PMCID: PMC6400661.

14: Yu X, Zhao X, Zhang J, Li Y, Sheng P, Ma C, Zhang L, Hao X, Zheng X, Xing Y, Qiao H, Qu L, Zhu D. Dacomitinib, a new pan-EGFR inhibitor, is effective in attenuating pulmonary vascular remodeling and pulmonary hypertension. Eur J Pharmacol. 2019 May 5;850:97-108. doi: 10.1016/j.ejphar.2019.02.008. Epub 2019 Feb 10. PubMed PMID: 30753867.

15: Qiu X, Lin Q, Ning Z, Qian X, Li P, Ye L, Xie S. Quantitative bioanalytical assay for the human epidermal growth factor receptor (HER) inhibitor dacomitinib in rat plasma by UPLC-MS/MS. J Pharm Biomed Anal. 2019 Mar 20;166:66-70. doi: 10.1016/j.jpba.2018.12.041. Epub 2018 Dec 28. PubMed PMID: 30612075.

16: Shirley M. Dacomitinib: First Global Approval. Drugs. 2018 Dec;78(18):1947-1953. doi: 10.1007/s40265-018-1028-x. Review. PubMed PMID: 30506139.

17: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from http://www.ncbi.nlm.nih.gov/books/NBK532497/ PubMed PMID: 30372001.

18: Dacomitinib Approved, but Might Not Be Used. Cancer Discov. 2018 Dec;8(12):1500. doi: 10.1158/2159-8290.CD-NB2018-138. Epub 2018 Oct 25. PubMed PMID: 30361446.

19: Sepúlveda JM, Sánchez-Gómez P, Vaz Salgado MÁ, Gargini R, Balañá C. Dacomitinib: an investigational drug for the treatment of glioblastoma. Expert Opin Investig Drugs. 2018 Oct;27(10):823-829. doi: 10.1080/13543784.2018.1528225. Epub 2018 Oct 5. Review. PubMed PMID: 30247945.

20: Mok TS, Cheng Y, Zhou X, Lee KH, Nakagawa K, Niho S, Lee M, Linke R, Rosell R, Corral J, Migliorino MR, Pluzanski A, Sbar EI, Wang T, White JL, Wu YL. Improvement in Overall Survival in a Randomized Study That Compared Dacomitinib With Gefitinib in Patients With Advanced Non-Small-Cell Lung Cancer and EGFR-Activating Mutations. J Clin Oncol. 2018 Aug 1;36(22):2244-2250. doi: 10.1200/JCO.2018.78.7994. Epub 2018 Jun 4. PubMed PMID: 29864379.