Solubility
ChemicalBook > CAS DataBase List > Larotrectinib Sulfate

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;Larotinib sulfate;LOXO-101 (sulfate);Larotrectinib sulfate;Larotrectinib(LOXO 101;ARRY-470, Larotrectinib;Larotrectinib sulfate salt
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

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
10003
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
159
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
479
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
4674
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
2024-12-12
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

1223405-08-0, Larotrectinib SulfateRelated Search:


  • 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)
  • Larotinib sulfate
  • 1223405-08-0
  • C21H24F2N6O6S
  • C21H22F2N6O2H2SO4
  • API
  • LOXO-101