パクリチニブ

パクリチニブ

Material name by the IUPAC glossology
IUPAC name (16E) -11-[2-(1-Pyrrolidinyl)ethoxy] -14,19-dioxa-5,7,26-triazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene
Clinical data
Legal regulation	Under development
Dosage method	Oral
Identification
ATC cord	Unavailable
PubChem	CID: 46216796
ChemSpider	28518965
ChEMBL	CHEMBL2035187
Another name	SB1518
Chemical data
Chemical formula	C28H32N4O3
Molecular weight	472.58 g/mol
SMILES c1cc2cc(c1) -c3ccnc(n3)Nc4ccc(c(c4)COC/C=C/COC2)OCCN5CCCC5
InChI InChI=1S/C28H32N4O3/c1-2-13-32(12-1)14-17-35-27-9-8-25-19-24(27)21-34-16-4-3-15-33-20-22-6-5-7-23(18-22)26-10-11-29-28(30-25)31-26/h3-11,18-19H,1-2,12-17,20-21H2,(H,29,30,31)/b4-3+ Key:HWXVIOGONBBTBY-ONEGZZNKSA-N

パクリチニブ (Pacritinib, INN ^[1]) Oh, it is the ringed Janus kinase repressor that development is pushed forward as an osteomyelofibrosis therapeutic drug. I inhibit Janus kinase 2 (JAK2) mainly. A clinical third aspect examination was conducted in 2013 [²].

This medicine was discovered in Singaporean S* bio Pte Ltd. It was IC₅₀=19 nM, and the JAK2 inhibitory activity had good selectivity for IC₅0 = 23 nM, JAK2 V617F variation for JAK2 wild type. Was IC₅0 =520nM in IC₅₀=1280 nM, JAK3 in JAK1 [³]; [⁴].

This drug is acquired by Cell Therapeutics, Inc. (CTI) and Baxter, and development is pushed forward toward an osteomyelofibrosis patient presenting with thrombocytopenia with other JAK repressors [⁵].

Reference materials

1. ^ "International Nonproprietary Names for Pharmaceutical Substances (INN) List 104." WHO Drug Information 24 (4): 386. (2010). http://apps.who.int/iris/bitstream/10665/74579/1/24_4_2010_INN104.pdf. 
2. ^ "JAK-Inhibitoren: Neue Wirkstoffe für viele Indikationen" (German). Pharmazeutische Zeitung (21). (2013). http://www.pharmazeutische-zeitung.de/index.php?id=46539. 
3. ^ William, A. D.; Lee, A. C. -H.; Blanchard, S. P.; Poulsen, A.; Teo, E. L.; Nagaraj, H.; Tan, E.; Chen, D. et al. (2011). "Discovery of the Macrocycle 11-(2-Pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a Potent Janus Kinase 2/Fms-Like Tyrosine Kinase-3 (JAK2/FLT3) Inhibitor for the Treatment of Myelofibrosis and Lymphoma." Journal of Medicinal Chemistry 54 (13): 4638–58. doi: 10.1021/jm200326p. PMID 21604762. 
4. ^ Poulsen, A.; William, A.; Blanchard, S. P.; Lee, A.; Nagaraj, H.; Wang, H.; Teo, E.; Tan, E. et al. (2012). "Structure-based design of oxygen-linked macrocyclic kinase inhibitors: Discovery of SB1518 and SB1578, potent inhibitors of Janus kinase 2 (JAK2) and Fms-like tyrosine kinase-3 (FLT3)." Journal of Computer-Aided Molecular Design 26 (4): 437–50. doi: 10.1007/s10822-012-9572-z. PMID 22527961. 
5. ^ Baxter licenses cancer drug from CTI in $172m deal

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