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2018 Korea CPHI, C30
LOXO-195 is a potent and selective TRK inhibitor capable of addressing potential mechanisms of acquired resistance that may emerge in patients receiving larotrectinib (LOXO-101) or multikinase inhibitors with anti-TRK activity. LOXO-195 demonstrated potent inhibition of TRK fusions, including critical acquired resistance mutations, in enzyme and cellular assays, with minimal activity against other kinases. In diverse TRK fusion mouse models, LOXO-195 inhibited phospho-ERK and caused dramatic tumor growth inhibition, superior to first generation TRK inhibitors, without significant toxicity
LOXO-195 , CAS#1350884-56-8, HNMR, HPLC 99%+, LCMS, COA, MSDS and ROS, more than 20G in stock, pls check:
Name:LOXO-195
CAS#: 1350884-56-8
Formula: C20H21FN6O
Exact Mass: 380.1761
Molecular Weight: 380.4274
Elemental Analysis: C, 63.14; H, 5.56; F, 4.99; N, 22.09; O, 4.21
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Formula: C20H21FN6O
Exact Mass: 380.1761
Molecular Weight: 380.4274
Elemental Analysis: C, 63.14; H, 5.56; F, 4.99; N, 22.09; O, 4.21
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Synonym: LOXO-195; LOXO 195; LOXO195.
IUPAC/Chemical Name: (13E,14E,22R,6R)-35-fluoro-6-methyl-7-aza-1(5,3)-pyrazolo[1,5-a]pyrimidina-3(3,2)-pyridina-2(1,2)-pyrrolidinacyclooctaphan-8-one
InChi Key: OEBIHOVSAMBXIB-SJKOYZFVSA-N
InChi Code: InChI=1S/C20H21FN6O/c1-12-4-5-16-14(9-13(21)10-22-16)17-3-2-7-26(17)18-6-8-27-19(25-18)15(11-23-27)20(28)24-12/h6,8-12,17H,2-5,7H2,1H3,(H,24,28)/t12-,17-/m1/s1
SMILES Code: FC1=CN=C(CC[C@@H](C)NC(C2=C3N(C=CC4=N3)N=C2)=O)C([C@@H]5N4CCC5)=C1
Reference：
Can·cer, redefined
Lisa M. Jarvis
C&EN Global Enterp, 2017, 95 (27), pp 26–30
Publication Date (Web): July 3, 2017 (Article)
DOI: 10.1021/cen-09527-cover
