ChemicalBook > CAS DataBase List > LOXO-292

LOXO-292

Binding Mode

Product Name: LOXO-292
CAS No.: 2152628-33-4
Chemical Name: LOXO-292
Synonyms: SELPERCATINIB;LOX-292;CPD2206;LOX0292;Orapani;LOXO-292;ARRY-192);Secatinib;Serpatinib;Selpercatinib API
CBNumber: CB34805442
Molecular Formula: C29H31N7O3
Formula Weight: 525.6
MOL File: 2152628-33-4.mol

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LOXO-292 Property

Density: 1.36±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO:20.0(Max Conc. mg/mL);38.05(Max Conc. mM)
form: A crystalline solid
pka: 14.00±0.29(Predicted)
color: White to off-white
InChI: InChI=1S/C29H31N7O3/c1-29(2,37)18-39-24-9-25(28-21(10-30)13-33-36(28)17-24)20-5-6-26(31-12-20)34-15-22-8-23(16-34)35(22)14-19-4-7-27(38-3)32-11-19/h4-7,9,11-13,17,22-23,37H,8,14-16,18H2,1-3H3
InChIKey: XIIOFHFUYBLOLW-UHFFFAOYSA-N
SMILES: C12=C(C#N)C=NN1C=C(OCC(O)(C)C)C=C2C1=CC=C(N2CC3CC(N3CC3=CC=C(OC)N=C3)C2)N=C1

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0084279
Product name: Selpercatinib
Purity: 99.87%
Packaging: 5mg
Price: $250
Updated: 2021/12/16

ChemScene

Product number: CS-0084279
Product name: Selpercatinib
Purity: 99.87%
Packaging: 10mg
Price: $350
Updated: 2021/12/16

ChemScene

Product number: CS-0084279
Product name: Selpercatinib
Purity: 99.87%
Packaging: 50mg
Price: $1100
Updated: 2021/12/16

Biorbyt Ltd

Product number: orb573122
Product name: LOXO-292(Selpercatinib)
Purity: >98%
Packaging: 100mg
Price: $1283.5
Updated: 2021/12/16

ChemScene

Product number: CS-0084279
Product name: Selpercatinib
Purity: 99.87%
Packaging: 100mg
Price: $1800
Updated: 2021/12/16

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LOXO-292 Chemical Properties,Usage,Production

Binding Mode

In the co-crystal structure of selpercatinib-RET kinase, the pyrazolopyridine occupies the adenosine pocket, forming a direct hydrogen bond between N1 and amide NH of Ala807 and an indirect hydrogen bond between C6 ether oxygen and amide NH of Gly810 via a bound water molecule. In addition, one piperazine nitrogen also interact with one water molecule (Figs. 3, 4).

Uses

Selpercatinib(LOXO-292) is a highly selective, potent RET inhibitor, an oral drug used to treat cancers in people whose tumours have been altered (mutated or fused) in specific genes (RET stands for "rearrangement during transfection").

brand name

Retevmo

General Description

Class: receptor tyrosine kinase; Treatment: RET-altered lung/thyroid cancers; Other name: ARRY-192, LOXO-292; Oral bioavailability = 73%; Elimination half-life = 32 h; Protein binding = 97%

Side effects

LOXO-292(Selpercatinib) can cause serious side effects including liver toxicity, high blood pressure, heart rhythm changes due to prolongation of heart electrical activity (QT prolongation), bleeding, allergic reactions, impaired wound healing and harm to an unborn baby.

Synthesis

The sulfonyl chloride starting material 329 was reacted with tert-butyl hydroxyurea (330) under basic conditions and subsequently treated with trifluoroacetic acid (TFA) to afford O-sulfonylhydroxylamine 332. O-sulfonylhydroxylamine 332, as a nitrogen source, reacted with pyridine 333 to afford N-aminopyridinium salt 334. N-aminopyridinium salt 334 was further reacted with 2-chloroacrylonitrile (335) to establish the pyrazolopyridine core 336. Removal of the methyl ether using dodecanethiol (337) in warm dimethylformamide under basic conditions afforded the phenolic compound 338. Phenol 338 was converted to the triflate (339). The triflate 339 was cross-coupled with the boronate ester 340 under Suzuki conditions to react specifically at the triflate position with retention of the bromide to afford 341. 341 was reacted with the epoxide 342 under palladium catalysis to establish the ether side chain. Finally, the azabicyclic addendum 344 was installed via an NMR aromatic substitution reaction to generate salacartinib in 86% yield.

target

RET

storage

Store at -20°C

Dosage

The recommended selpercatinib dose based on body weight is: (1) Less than 50 kg: 120 mg orally twice daily (2) 50 kg or greater: 160 mg orally twice daily

LOXO-292 Preparation Products And Raw materials

Raw materials

Preparation Products

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LOXO-292 Suppliers

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View Lastest Price from LOXO-292 manufacturers

Zison Pharmaceutical (Shandong) Co., Ltd.

Product: Selpercatinib 2152628-33-4
Price: US $0.00-0.00/kg
Min. Order: 1kg
Purity: ＞99.5% by HPLC
Supply Ability: 100kg/month
Release date: 2023-02-18

Jinan Million Pharmaceutical Co., Ltd

Product: Selpercatinib(LOXO-292) 2152628-33-4
Price: US $2.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 30KG/M
Release date: 2023-08-15

HangZhou RunYan Pharma Technology Co.,LTD.

Product: Selpercatinib; Loxo-292 2152628-33-4
Price: US $0.00-0.00/MG
Min. Order: 10MG
Purity: 99% HPLC
Supply Ability: 10000
Release date: 2024-09-19

2152628-33-4, LOXO-292Related Search:

LOXO-195 Selumetinib Saracatinib LOXO-292 2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)Methyl)benzoic acid 4-Chloro-7H-pyrrolo[2,3-d]pyrimidine 2-Amino-6-bromopyridine Brigatinib Crizotinib 5-Formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic acid Lorlatinib (PF-06463922) Olaparib Glecaprevir ABT-530 NBQX DISODIUM SALT SU14813 S-Ruxolitinib (INCB018424) Futibatinib

CPD2206

LOX-292

LOXO-292; LOXO292;LOXO 292

LOXO-292,Selpercatinib

Selpercatinib(LOXO-292)

6-?(2-?Hydroxy-?2-?methylpropoxy)?-?4-?[6-?[6-?[(6-?methoxy-?3-?pyridinyl)?methyl]?-?3,?6-?diazabicyclo[3.1.1]?hept-?3-?yl]?-?3-?pyridinyl]?pyrazolo[1,?5-?a]?pyridine-?3-?carbonitrile

Pyrazolo[1,5-a]pyridine-3-carbonitrile, 6-(2-hydroxy-2-methylpropoxy)-4-[6-[6-[(6-methoxy-3-pyridinyl)methyl]-3,6-diazabicyclo[3.1.1]hept-3-yl]-3-pyridinyl]-

LOXO-292 USP/EP/BP

6-(2-hydroxy-2-methylpropoxy)-4-[6-[6-[(6-methoxypyridin-3-yl)methyl]-3,6-diazabicyclo[3.1.1]heptan-3-yl]pyridin-3-yl]pyrazolo[1,5-a]pyridine-3-carbonitrile

Inhibitor LOXO-292

ARRY-192)

Selpercatinib (LOXO-292, ARRY-192)

LOX0292

Serpatinib

SELPERCATINIB

LOXO-292

13C,2H3]-Selpercatinib

Diethyl N-[5-[N-[(3,4-dihydro-2-methyl-4-oxo-6-quinazolinyl) methyll-N-methylamino]-2-thenoyll-L-glutamate

Orapani

Selpatinib LOXO-292

Selpercatinib API

Selpercatinib, 10 mM in DMSO

Secatinib

2152628-33-4

API

2152628-33-4