Original:Olmutinib free base1353550-13-6 , stock more than 100g

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Description: Olmutinib, also known as HM61713 and BI-1482694, is a potent small molecule inhibitor of Bruton's tyrosine kinase (BTK). BTK is a member of the Tec family of non-receptor protein tyrosine kinases. BTK is mostly expressed in hematopoietic cells such as B cells, mast cells and macrophages. BTK plays key roles in multiple cell signaling pathways including B-Cell Receptor (BCR) and Fc receptor (FcR) signaling cascades and is an essential mediator not only in B-cell dependent but also in myeloid cell dependent inflammatory arthritis. HM71224 has been selected as a novel therapeutic agent for the treatment of autoimmune diseases such as RA.

Name: Olmutinib free base 

CAS#: 1353550-13-6 (free base) 

Chemical Formula: C26H26N6O2S 

Exact Mass: 486.18379 

Molecular Weight: 486.59 

Elemental Analysis: C, 64.18; H, 5.39; N, 17.27; O, 6.58; S, 6.59

Synonym: HM61713; HM 61713; HM-61713; BI 1482694; BI-1482694; BI1482694; Olmutinib.

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

InChi Key: FDMQDKQUTRLUBU-UHFFFAOYSA-N

InChi Code: InChI=1S/C26H26N6O2S/c1-3-23(33)27-19-5-4-6-21(17-19)34-25-24-22(11-16-35-24)29-26(30-25)28-18-7-9-20(10-8-18)32-14-12-31(2)13-15-32/h3-11,16-17H,1,12-15H2,2H3,(H,27,33)(H,28,29,30)

SMILES Code: C=CC(NC1=CC=CC(OC2=C3C(C=CS3)=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1)=O

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).

Harmonized System Code: 293490

ADDITIONAL INFORMATION

Related CAS# 

1353550-13-6 (free base); 1842366-97-5 (HCl). 

1802181-20-9 (deleted CAS#)

Note: Olmutinib was previously mistakely cited as "HM71224". As of 9/12/2016, there are many vendor still cit 

  

  

REFERENCES

1: Park K, Han JY, Kim DW, Bazhenova LA, Ou SH, Pang YK, Hin HS, Juan O, Son J, Jänne P. 190TiP: ELUXA 1: Phase II study of BI 1482694 (HM61713) in patients (pts) with T790M-positive non-small cell lung cancer (NSCLC) after treatment with an epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI). J Thorac Oncol. 2016 Apr;11(4 Suppl):S139. doi: 10.1016/S1556-0864(16)30299-4. Epub 2016 Apr 15. PubMed PMID: 27198328.

2: Park K, Lee JS, Han JY, Lee KH, Kim JH, Cho EK, Cho JY, Min YJ, Kim JS, Kim DW. 1300: Efficacy and safety of BI 1482694 (HM61713), an EGFR mutant-specific inhibitor, in T790M-positive NSCLC at the recommended phase II dose. J Thorac Oncol. 2016 Apr;11(4 Suppl):S113. doi: 10.1016/S1556-0864(16)30243-X. Epub 2016 Apr 15. PubMed PMID: 27198272.

3: Wang S, Cang S, Liu D. Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer. J Hematol Oncol. 2016 Apr 12;9:34. doi: 10.1186/s13045-016-0268-z. Review. PubMed PMID: 27071706; PubMed Central PMCID: PMC4830020.

4: Tan CS, Cho BC, Soo RA. Next-generation epidermal growth factor receptor tyrosine kinase inhibitors in epidermal growth factor receptor -mutant non-small cell lung cancer. Lung Cancer. 2016 Mar;93:59-68. doi: 10.1016/j.lungcan.2016.01.003. Epub 2016 Jan 8. Review. PubMed PMID: 26898616.

5: Song HN, Jung KS, Yoo KH, Cho J, Lee JY, Lim SH, Kim HS, Sun JM, Lee SH, Ahn JS, Park K, Choi YL, Park W, Ahn MJ. Acquired C797S Mutation upon Treatment with a T790M-Specific Third-Generation EGFR Inhibitor (HM61713) in Non-Small Cell Lung Cancer. J Thorac Oncol. 2016 Apr;11(4):e45-7. doi: 10.1016/j.jtho.2015.12.093. Epub 2015 Dec 31. PubMed PMID: 26749488.

6: Pirker R. Third-generation epidermal growth factor receptor tyrosine kinase inhibitors in advanced nonsmall cell lung cancer. Curr Opin Oncol. 2016 Mar;28(2):115-21. doi: 10.1097/CCO.0000000000000260. PubMed PMID: 26720671.

7: Ou SH, Soo RA. Dacomitinib in lung cancer: a "lost generation" EGFR tyrosine-kinase inhibitor from a bygone era? Drug Des Devel Ther. 2015 Oct 15;9:5641-53. doi: 10.2147/DDDT.S52787. eCollection 2015. Review. PubMed PMID: 26508839; PubMed Central PMCID: PMC4610796.

8: Tartarone A, Lerose R. Clinical approaches to treat patients with non-small cell lung cancer and epidermal growth factor receptor tyrosine kinase inhibitor acquired resistance. Ther Adv Respir Dis. 2015 Oct;9(5):242-50. doi: 10.1177/1753465815587820. Epub 2015 May 27. Review. PubMed PMID: 26016841.

9: Wang H, Guo R, Zhang L. [TKI Resistance for T790M Mutation]. Zhongguo Fei Ai Za Zhi. 2015 Apr;18(4):245-50. doi: 10.3779/j.issn.1009-3419.2015.04.10. Review. Chinese. PubMed PMID: 25936890.

10: Liao BC, Lin CC, Yang JC. Second and third-generation epidermal growth factor receptor tyrosine kinase inhibitors in advanced nonsmall cell lung cancer. Curr Opin Oncol. 2015 Mar;27(2):94-101. doi: 10.1097/CCO.0000000000000164. Review. PubMed PMID: 25611025.

11: Stinchcombe TE. Recent advances in the treatment of non-small cell and small cell lung cancer. F1000Prime Rep. 2014 Dec 1;6:117. doi: 10.12703/P6-117. eCollection 2014. Review. PubMed PMID: 25580271; PubMed Central PMCID: PMC4251418.

12: Steuer CE, Khuri FR, Ramalingam SS. The next generation of epidermal growth factor receptor tyrosine kinase inhibitors in the treatment of lung cancer. Cancer. 2015 Apr 15;121(8):E1-6. doi: 10.1002/cncr.29139. Epub 2014 Dec 17. Review. PubMed PMID: 25521095.

13: Peters S, Zimmermann S, Adjei AA. Oral epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of non-small cell lung cancer: comparative pharmacokinetics and drug-drug interactions. Cancer Treat Rev. 2014 Sep;40(8):917-26. doi: 10.1016/j.ctrv.2014.06.010. Epub 2014 Jul 1. PubMed PMID: 25027951.