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LOXO-101

LOXO-101 Structure
CAS No.
1223403-58-4
Chemical Name:
LOXO-101
Synonyms
Larotrectinib;Larotrec;LOXO-101,LAROTRECTINIB,ARRY-470 (LAROTRECTINIB SULFATE CAS:1223405-08-0);(3S)-N-[5-[(2R)-2-(2,5-Difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-1-pyrrolidinecarboxamide;CS-2322;LOXO 10;ARRY 470;LOXO-101;ROM for Nepal;LOXO101;LOXO 101
CBNumber:
CB53121981
Molecular Formula:
C21H22F2N6O2
Molecular Weight:
428.44
MOL File:
1223403-58-4.mol
Modify Date:
2024/5/23 14:10:19
Request For Quotation

LOXO-101 Properties

Density 1.55±0.1 g/cm3(Predicted)
storage temp. RT
solubility Soluble in DMSO (up to 5 mg/ml).
form solid
pka 8.41±0.40(Predicted)
color Yellow
Stability Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302-H317
Precautionary statements  P280

LOXO-101 Chemical Properties,Uses,Production

Description

LOXO-101 is an inhibitor of the tropomyosin-related kinases TrkA, TrkB, and TrkC (IC50s = 2-20 nM). It is selective for TrkA, -B, and -C over a panel of 226 kinases at 1 μM. LOXO-101 inhibits the growth of CUTO-3.29, KM12, and MO-91 patient-derived cancer cell lines (IC50s = <100, <10, and <10 nM, respectively). In vivo, LOXO-101 (60 and 200 mg/kg) reduces tumor growth in a KM12 mouse xenograft model.

Description

Larotrectinib, also known as LOXO-101 and ARRY-470, is a small molecule that was designed to block the ATP-binding site of the TRKA, TRKB, and TRKC, serving as a highly specific and potent inhibitor of all of the three tropomyosin kinase receptors.

Uses

Larotrectinib is a TRK Inhibitor (Tyrosine kinase inhibitor).

brand name

Vitrakvi

General Description

Class: receptor tyrosine kinase; Treatment: NTRK-altered solid tumors; Other name: ARRY-407, LOXO-101; Oral bioavailability = 25%; Elimination half-life = 2.9 h; Protein binding = 70%

Clinical Use

The US Food and Drug Administration (FDA) granted accelerated approval to larotrectinib (Vitrakvi?) on November 26th, 2018, as a treatment for adult and pediatric patients with solid tumors that have NTRK gene fusions without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and have no satisfactory alternative treatments or that have progressed following treatment on. In the approval statement by FDA, a complete response rate of 22% and partial response rate of 53% were cited.

target

pan-TRK

LOXO-101 Preparation Products And Raw materials

Raw materials

Preparation Products

Larotrectinib Sulfate

LOXO-101 Suppliers

Global( 207)Suppliers
Supplier Tel Country ProdList Advantage Inquiry
Pharma Affiliates 172-5066494 Haryana, India 6761 58 Inquiry
SynZeal Research Pvt Ltd +1 226-802-2078 Gujarat, India 6522 58 Inquiry
Pharmaffiliates Analytics and Synthetics P. Ltd +91-172-5066494 Haryana, India 6773 58 Inquiry
CLEARSYNTH LABS LTD. +91-22-45045900 Hyderabad, India 6351 58 Inquiry
Hebei Yanxi Chemical Co., Ltd. +86-17531190177; +8617531190177 China 6011 58 Inquiry
shandong perfect biotechnology co.ltd +86-53169958659; +8618596095638 China 294 58 Inquiry
Henan Tianfu Chemical Co.,Ltd. +86-0371-55170693 +86-19937530512 China 21676 55 Inquiry
Hangzhou FandaChem Co.,Ltd. 008657128800458; +8615858145714 China 9338 55 Inquiry
ATK CHEMICAL COMPANY LIMITED +undefined-21-51877795 China 32760 60 Inquiry
career henan chemical co +86-0371-86658258 +8613203830695 China 29901 58 Inquiry
Supplier Advantage
Pharma Affiliates 58
SynZeal Research Pvt Ltd 58
Pharmaffiliates Analytics and Synthetics P. Ltd 58
CLEARSYNTH LABS LTD. 58
Hebei Yanxi Chemical Co., Ltd. 58
shandong perfect biotechnology co.ltd 58
Henan Tianfu Chemical Co.,Ltd. 55
Hangzhou FandaChem Co.,Ltd. 55
ATK CHEMICAL COMPANY LIMITED 60
career henan chemical co 58

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LOXO-101 (R)-N-(5-((S)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide ARRY 470 (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide LOXO-101 (ARRY-470) CS-2322 LOXO101;LOXO 101 LOXO-101 Larotrectinib LOXO-101 (ARRY-470,Larotrectinib) LOXO-101,LAROTRECTINIB,ARRY-470 Larotrectinib base 1-Pyrrolidinecarboxamide, N-[5-[(2R)-2-(2,5-difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-, (3S)- LOXO101（free base） ROM for Nepal LOXO 10 (3S)-N-{5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-yl}-3-hydroxypyrrolidine-1-carboxamide (3S)-N-[5-[(2R)-2-(2,5-Difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-1-pyrrolidinecarboxamide Larotrectinib LOXO-101,LAROTRECTINIB,ARRY-470 (LAROTRECTINIB SULFATE CAS:1223405-08-0) Larotrec LarotrectinibFor 1223403-58-4 1223403-66-1 C21H22F2N6O2 API APIs