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
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
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.
N-Bromosuccinimide Price
- Product number
- CS-0084279
- Product name
- Selpercatinib
- Purity
- 99.87%
- Packaging
- 5mg
- Price
- $250
- Updated
- 2021/12/16
- Product number
- CS-0084279
- Product name
- Selpercatinib
- Purity
- 99.87%
- Packaging
- 10mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0084279
- Product name
- Selpercatinib
- Purity
- 99.87%
- Packaging
- 50mg
- Price
- $1100
- Updated
- 2021/12/16
- Product number
- orb573122
- Product name
- LOXO-292(Selpercatinib)
- Purity
- >98%
- Packaging
- 100mg
- Price
- $1283.5
- Updated
- 2021/12/16
- Product number
- CS-0084279
- Product name
- Selpercatinib
- Purity
- 99.87%
- Packaging
- 100mg
- Price
- $1800
- Updated
- 2021/12/16
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
LOXO-292 Suppliers
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View Lastest Price from LOXO-292 manufacturers
- 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
- 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
- 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