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LOXO-195

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LOXO-195 Basic information

Product Name:
LOXO-195
Synonyms:
  • (3aR,10R)-5-Fluoro-1,2,3,3a,8,9,10,11-octahydro-10-methyl-12H-15,17-ethenopyrazolo[3,4-d]pyrido[2,3-k]pyrrolo[2,1-m][1,3,7]triazacyclotridecin-12-one
  • selitrectinib（LOXO-195）
  • CS-2800
  • LOXO-195;LOXO195
  • Selitrectinib
  • LOXO 195(Selitrectinib)
  • Selitrectinib (Synonyms: LOXO-195)
  • 12H-15,17-Ethenopyrazolo[3,4-d]pyrido[2,3-k]pyrrolo[2,1-m][1,3,7]triazacyclotridecin-12-one, 5-fluoro-1,2,3,3a,8,9,10,11-octahydro-10-methyl-, (3aR,10R)-
CAS:
2097002-61-2
MF:
C20H21FN6O
MW:
380.42
Mol File:
2097002-61-2.mol
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LOXO-195 Chemical Properties

Density 
1.51±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:62.5(Max Conc. mg/mL);164.29(Max Conc. mM)
form 
A crystalline solid
pka
11.44±0.40(Predicted)
color 
White to yellow
InChI
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
InChIKey
OEBIHOVSAMBXIB-SJKOYZFVSA-N
SMILES
N12CCC[C@]1([H])C1=CC(F)=CN=C1CC[C@@H](C)NC(=O)C1C=NN3C=CC2=NC=13
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Safety Information

HS Code 
2933998090
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LOXO-195 Usage And Synthesis

Uses

LOXO-195 (Selitrectinib) is a second-generation TRK kinase inhibitor that targets TRK fusion-positive tumors and is used to treat tumor patients who are resistant to first-generation TRK inhibitors.

in vivo

Stably transfected NIH-3T3 ΔTRKA and ΔTRKA-G595R cells are implanted subcutaneously into the flanks of nude mice. Both larotrectinib and Selitrectinib (LOXO-195) are effective at reducing phosphorylated TRKA in tumors driven by ΔTRKA. In contrast, only Selitrectinib (LOXO-195) strongly suppresses phospho-TRKA in ΔTRKA-G595R cells in a dose-dependent manner. Selitrectinib (LOXO-195) also causes inhibition of tumor growth relative to vehicle at all doses in four TRKA-dependent tumor models (ΔTRKA, ΔTRKA-G595R, ΔTRKAG667C, and TPM3-NTRK1 fusion-positive KM12 colorectal cancer cells. Larotrectinib inhibits KM12 and NIH 3T3-ΔTRKA tumors to a similar degree. Group mean body weight loss does not exceed 5% for any agent. Selitrectinib (LOXO-195) displays high selectivity for the TRK proteins[1]

IC 50

TrkA: 0.6 nM (IC50); TrkC: <2.5 nM (IC50)

LOXO-195Supplier

Changzhou Fulangke Chemical Technology Co., Ltd. Gold
Tel
13776872728
Email
amwpl888@sina.cn
Hubei Kele Fine Chemical Co., Ltd Gold
Tel
027-59101668 19945030958
Email
2881924765@qq.com
TargetMol Chemicals Inc. Gold
Tel
021-021-33632979 15002134094
Email
marketing@targetmol.com
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Shanghai Topbiochem Technology Co., Ltd
Tel
021-58170097
Email
info@topbiochem.com
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