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執大象，天下往，往而無害，安平泰
WEB: www.eosmedchem.com
EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com
TEL: 0086-531-69905422
GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.
Description: Larotrectinib, also known as ARRY-470 and LOXO-101, is an orally bioavailable, potent, ATP-competitive inhibitor of TRKA, TRKB, and TRKC. LOXO-101 has IC50 values in the low nanomolar range for inhibition of all three TRK family members in binding and cellular assays, with 100x selectivity over other kinases, and has shown acceptable pharmaceutical properties and safety in nonclinical models. The TRK family of neurotrophin receptors, TRKA, TRKB, and TRKC (encoded by NTRK1, NTRK2, and NTRK3 genes, respectively) and their neurotrophin ligands regulate growth, differentiation and survival of neurons.
Name: LOXO-101 (ARRY-470)
CAS#: 1223403-58-4
Chemical Formula: C21H22F2N6O2
Exact Mass: 428.17723
Molecular Weight: 428.44
Elemental Analysis: C, 58.87; H, 5.18; F, 8.87; N, 19.62; O, 7.47
Synonym: LOXO 101; LOXO-101; LOXO101; ARRY-470; ARRY470; ARRY 470; larotrectinib
IUPAC/Chemical Name: (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
InChi Key: NYNZQNWKBKUAII-KBXCAEBGSA-N
InChi Code: InChI=1S/C21H22F2N6O2/c22-13-3-4-16(23)15(10-13)18-2-1-7-28(18)19-6-9-29-20(26-19)17(11-24-29)25-21(31)27-8-5-14(30)12-27/h3-4,6,9-11,14,18,30H,1-2,5,7-8,12H2,(H,25,31)/t14-,18+/m0/s1
SMILES Code: O=C(N1CC[C@@H](C1)O)NC2=C3N=C(N4CCC[C@@H]4C5=CC(F)=CC=C5F)C=CN3N=C2
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
REFERENCES
Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang, Substituted pyrazolo[1,5-a]pyrimidine compounds as Trk kinase inhibitors and their preparation and use in the treatment of diseases. WO2010048314 (2010).
