LOXO-101
1223403-58-4
industrial Grade
98%
SHANGHAI
KieRay Chem
25kg/drum
2022-12-31
fine chemicals,pharmaceutical materials
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Product Description
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Seller Information
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DescriptionECHEMI Editorial ReferenceLarotrectinib (VITRAKVIR) is an orally administered, small molecule, highly-selective, tropomyosin receptor kinase (TRK) inhibitor that was developed by Loxo Oncology in collaboration with Bayer AG as a treatment for adult and paediatric patients whose cancers harbour neurotrophic receptor tyrosine kinase (NTRK) gene fusions.Larotrectinib is a highly selective, potent inhibitor of TRKA, TRKB and TRKC (in vitro 50% inhibitory constant 5–11 nmol/L), with minimal or no activity against other kinase and non-kinase targets [1, 2]. Inhibition of TRKs prevents TRK activation, resulting in both the induction of cellular apoptosis and the inhibition of cell growth in tumours that overexpress TRKs.
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.
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.
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%Basic Info-
Product Name:
LOXO-101
Other Name:LOXO-101;CS-2322;LOXO101;LOXO 101;LOXO-101 Larotrectinib;LOXO-101 (ARRY-470,Larotrectinib);LOXO-101,LAROTRECTINIB,ARRY-470;ARRY 470;(S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
CAS No.:1223403-58-4
Molecular Formula:C21H22F2N6O2
InChIKeys:InChIKey=NYNZQNWKBKUAII-KBXCAEBGSA-N
Molecular Weight:428.44
Exact Mass:428.44
Color/Form:Yellow
Categories:
Characteristics-
PSA:
86
XLogP3:3.0234
Appearance:White to yellow solid
Density:1.55±0.1 g/cm3(Predicted)
PKA:8.41±0.40(Predicted)
Critical Temperature & Pressure:RT
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Seller Information
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Business Type:
Manufactory
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Main Products:
fine chemicals,pharmaceutical materials
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Location:
Room 260, Building 3, No. 76 Xingqiao North Road, Xingqiao Street, Yuhang District, Hangzhou City, Zhejiang Province, China
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Payment Terms:
TT against copy of documents,L/C
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Average lead Time:
15 days
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Total Annual Revenue:
$1 million-$2.5 million
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Total Employees:
11-50
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Year of Establishment:
2020
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Country Product Purchase Quantity Date Posted Post an enquiry for this product
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