Larotrectinib Sulfate

Solubility

Product Name: Larotrectinib Sulfate
CAS No.: 1223405-08-0
Chemical Name: Larotrectinib Sulfate
Synonyms: LOX-101;Loxo-101（S）;LOX-101(sulfate);ARRY 470) sulfate;LOXO-101 (sulfate);Larotrectinib sulfate;Larotrectinib(LOXO 101;ARRY-470, Larotrectinib;Larotrectinib sulfate salt;Larotrectinib sulfate（LOXO101）
CBNumber: CB93067010
Molecular Formula: C21H24F2N6O6S
Formula Weight: 526.52
MOL File: 1223405-08-0.mol

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Larotrectinib Sulfate Property

storage temp.: Store at -20°C
solubility: ≥18.47 mg/mL in DMSO; ≥2.14 mg/mL in EtOH; ≥29.65 mg/mL in H2O
form: solid
color: Light yellow to brown
Stability:: Hygroscopic
InChI: InChI=1/C21H22F2N6O2.H2O4S/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;1-5(2,3)4/h3-4,6,9-11,14,18,30H,1-2,5,7-8,12H2,(H,25,31);(H2,1,2,3,4)/t14-,18+;/s3
InChIKey: PXHANKVTFWSDSG-RZOMTXEQNA-N
SMILES: S(O)(O)(=O)=O.FC1C=CC(F)=CC=1[C@H]1CCCN1C1C=CN2N=CC(NC(N3C[C@@H](O)CC3)=O)=C2N=1 |&1:13,29,r|

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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.

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

TRC

Product number: L175933
Product name: LarotrectinibSulfate
Packaging: 100mg
Price: $55
Updated: 2021/12/16

ChemScene

Product number: CS-5314
Product name: Larotrectinibsulfate
Purity: 99.69%
Packaging: 5mg
Price: $60
Updated: 2021/12/16

ApexBio Technology

Product number: B6176
Product name: LOXO-101
Packaging: 5mg
Price: $68
Updated: 2021/12/16

Biosynth Carbosynth

Product number: BL161518
Product name: Larotrectinib sulphate
Packaging: 10mg
Price: $90
Updated: 2021/12/16

ChemScene

Product number: CS-5314
Product name: Larotrectinibsulfate
Purity: 99.69%
Packaging: 10mg
Price: $100
Updated: 2021/12/16

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Larotrectinib Sulfate Chemical Properties,Usage,Production

Solubility

LOXO-101 (sulfate) can be dissolved in DMSO(Slightly), Methanol (Slightly, Sonicated), Water (Slightly) .

Description

LOXO-101 (sulfate) (or Larotrectinib Sulfate) 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.

Uses

Larotrectinib Sulfate is a potent and selective oral ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).

Clinical Use

Larotrectinib sulfate is approved to treat solid tumors with NTRKgene fusion without drug resistance mutation in specific TRK proteins. It is used in adults and children whose cancer has metastasized (spread to other parts of the body) or cannot be removed by surgery and has gotten worse after other treatments or cannot be treated with other therapies. This use is approved under FDA’s Accelerated Approval Program. As a condition of approval, a confirmatory trial(s) must show that larotrectinib sulfate provides a clinical benefit in these patients. Larotrectinib sulfate is also being studied in treating other types of cancer.

in vitro

in previous study, loxo-101 was evaluated for off-target kinase enzyme inhibition against a panel of non-trk kinases at a concentration of 1,000 nm and atp concentrations around the km. results showed that loxo-101 had greater than 50% inhibition for only one non-trk kinase, which was tnk2 with ic50 of 576 nm. moreover, there were neither relevant herg inhibition nor prolonged qt observation [1].

in vivo

animal study found that loxo-101 was able to inhibit in vivo tumor growth. athymic nude mice injected with km12 cells were orally treated with loxo-101 daily for 2 weeks, and dose-dependent tumor inhibition was observed, indicating the ability of loxo-101 to inhibit in-vivo tumor growth [1].

IC 50

low nanomolar range for inhibition of all trk family members

References

[1] doebele rc et al. an oncogenic ntrk fusion in a patient with soft-tissue sarcoma with response to the tropomyosin-related kinase inhibitor loxo-101. cancer discov.2015 oct;5(10):1049-57.

Larotrectinib Sulfate Preparation Products And Raw materials

Raw materials

Preparation Products

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Larotrectinib Sulfate Suppliers

China 172 India 2 United States 7 Global 181

Shanghai Subo Pharmaceutical Technology Co., Ltd.

Tel: 021-54156369 16621315851
Email: yhsuyiming@126.com
Country: China
ProdList: 310
Advantage: 58

Chunchuang (Wuhan) Technology Co., Ltd

Tel: 15342225168
Email: yutianchun2007@126.com
Country: China
ProdList: 10002
Advantage: 58

Shanghai Boyle Chemical Co., Ltd.

Tel
Fax: 86-21-57758967
Email: sales@boylechem.com
Country: China
ProdList: 2922
Advantage: 55

Chembest Research Laboratories Limited

Tel: +86-21-20908456
Fax: 021-58180499
Email: sales@BioChemBest.com
Country: China
ProdList: 6005
Advantage: 61

Anhui Lianchuang Biological Medicine Co.,Ltd

Tel: 0551-68779238 18056025720
Email: sales3@lcywhx.com
Country: China
ProdList: 158
Advantage: 57

Dalian Meilun Biotech Co., Ltd.

Tel: 0411-62910999 13889544652
Email: meilunui@163.com
Country: China
ProdList: 4727
Advantage: 58

Shanghai Hope Chem Co., Ltd.，

Tel: +21-18501659228 18501659228
Fax: sales@hope-chem.com
Email: info@hope-chem.com
Country: China
ProdList: 481
Advantage: 55

Haoyuan Chemexpress Co., Ltd.

Tel: 021-58950125
Fax: (86) 21-58955996
Email: info@chemexpress.com
Country: China
ProdList: 7552
Advantage: 61

Guangzhou Isun Pharmaceutical Co., Ltd

Tel: 020-39119399 18927568969
Fax: 020-39119999
Email: isunpharm@qq.com
Country: China
ProdList: 4428
Advantage: 55

TargetMol Chemicals Inc.

Tel: 021-021-33632979 15002134094
Fax: 021-33632979
Email: marketing@targetmol.com
Country: China
ProdList: 7783
Advantage: 58

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View Lastest Price from Larotrectinib Sulfate manufacturers

BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.

Product: Larotrectinib Sulfate 1223405-08-0
Price: US $0.00/g
Min. Order: 1g
Purity: More Than 99%
Supply Ability: 100kg/Month
Release date: 2024-07-23

Hebei Yanxi Chemical Co., Ltd.

Product: LOXO-101 (sulfate) 1223405-08-0
Price: US $0.00-0.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100tons
Release date: 2023-08-16

Zhuozhou Wenxi import and Export Co., Ltd

Product: LOXO-101 1223405-08-0
Price: US $15.00-10.00/KG
Min. Order: 1KG
Purity: 99%+ HPLC
Supply Ability: Monthly supply of 1 ton
Release date: 2021-07-09

1223405-08-0, Larotrectinib SulfateRelated Search:

PRND LOXO-101 BMN 673

LOXO-101 (sulfate)

(3S)-N-[5-[(2R)-2-(2,5-Difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-1-pyrrolidinecarboxamide sulfate (1:1)

Larotrectinib/LOXO 101/ARRY 470 sulfate

(3S)-N-[5-[(2R)-2-(2,5-Difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-1-pyrrolidinecarboxamide sulfate

ARRY 470) sulfate

Larotrectinib sulfate

Larotrectinib(LOXO 101

Larotrectinib (LOXO-101) sulfate

1-Pyrrolidinecarboxamide, N-[5-[(2R)-2-(2,5-difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-, (3S)-, sulfate (1:1)

ARRY-470, Larotrectinib

LOX-101

Loxo-101（S）

LOX-101(sulfate)

Larotrectinib sulfate（LOXO101）

(S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide sulfate

Larotrectinib sulfate salt

2H4]-Larotrectinib sulfate salt

LOXO-101 sulfate|||Larotrectinib (LOXO-101) sulfate|||Larotrectinib|||LOXO-101 (sulfate)|||ARRY-470|||ARRY-470 (sulfate)

1223405-08-0

C21H24F2N6O6S

C21H22F2N6O2H2SO4

API

LOXO-101