1223405-08-0
Larotrectinib sulfate
CAS: 1223405-08-0
Molecular Formula: C21H24F2N6O6S
1223405-08-0 - Names and Identifiers
1223405-08-0 - Physico-chemical Properties
| Molecular Formula | C21H24F2N6O6S |
| Molar Mass | 526.52 |
| Solubility | DMSO |
| Storage Condition | -20℃ |
| Physical and Chemical Properties | Bioactive Larotrectinib sulfate (LOXO-101, ARRY-470) is an oral, selective, ATP-competitive potent inhibitor of tropomyosin receptor kinase TRK. The inhibitory effect of Larotrectinib on TRKs can induce apoptosis and G1 cell cycle arrest. |
| Use | Uses (3S)-N-[5-[(2R)-2-(2, 5-difluorophenyl)-1-pyrrolidine] pyrazolo [1,5-A] pyrimidin-3-yl]-3-hydroxy-1-pyrrolidine formamide sulfate is a potent and selective oral ATP-competitive inhibitor of tropomyosin receptor kinase (TRK). |
| In vitro study | ARRY-470(LOXO-101) is a selective kinase inhibitor with molar grade activity on TRKA, TRKB and TRKC, while the inhibitory activity on other kinases is greater than 1000 nM. ARRY-470 does not inhibit the proliferation of Ba/F3 cells expressing other oncogenes (EGFR, ALK or ROS1), there was also no such effect on cell lines from the lung and colon that did not have NTRK1 fusions. ARRY-470(LOXO-101) can induce the apoptosis of kil-12 cells and arrest the cell cycle in the G1 phase. |
| In vivo study | Early sustained administration of ARRY-470(LOXO-101) significantly attenuated bone cancer pain, inhibited ectopic sprouting of sensory nerve fibers, and the formation of neuroma-like structures in tumor-bearing bone. However, there was no significant effect on tumor growth and bone remodeling. ARRY-470(LOXO-101) have very limited ability to cross the blood-brain barrier. |
1223405-08-0 - Upstream Downstream Industry
1223405-08-0 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.899 ml | 9.496 ml | 18.993 ml |
| 5 mM | 0.38 ml | 1.899 ml | 3.799 ml |
| 10 mM | 0.19 ml | 0.95 ml | 1.899 ml |
| 5 mM | 0.038 ml | 0.19 ml | 0.38 ml |
Last Update：2024-01-02 23:10:35
1223405-08-0 - Uses and synthesis methods
Target
Target Value
TRK
in vitro studies
ARRY-470(LOXO-101) is a selective kinase inhibitor with molar activity against TRKA, TRKB and TRKC, while its inhibitory activity against other kinases is greater than 1000 nM. ARRY-470 does not have a proliferation inhibitory effect on Ba/F3 cells expressing other oncogenes (epithelial growth factor receptor EGFR, ALK or ROS1), nor does it have this effect on cell lines from lung and colon that do not have NTRK1 fusion. ARRY-470(LOXO-101) can induce apoptosis of KM12 cells and arrest cell cycle in G1 phase.
In vivo studies
early continuous ARRY-470(LOXO-101) administration can significantly reduce bone cancer pain, inhibit ectopic germination of sensory nerve fibers and the formation of neuroma-like structures in tumor-bearing bones. But there is no significant effect on tumor growth and bone reconstruction. The ability of ARRY-470(LOXO-101) to cross the blood-brain barrier is very limited.
Last Update：2024-04-09 21:04:16
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CAS: 1223405-08-0
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CAS: 1223405-08-0
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Product Name: LOXO-101 (sulfate) Visit Supplier Webpage Request for quotation
CAS: 1223405-08-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1223405-08-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History
Raw Materials for 1223405-08-0
(S)-3-Hydroxypyrrolidine
5-(2,5-difluorophenyl)-3,4-dihydro-2H-pyrrole
3-nitropyrazolo[1,5-a]pyrimidin-5(4H)-one
LOXO-101
(2R)-2-(2,5-DIFLUOROPHENYL)PYRROLIDINE
1-Bromo-2,5-difluorobenzene
5-(2,5-difluorophenyl)-3,4-dihydro-2H-pyrrole
3-nitropyrazolo[1,5-a]pyrimidin-5(4H)-one
LOXO-101
(2R)-2-(2,5-DIFLUOROPHENYL)PYRROLIDINE
1-Bromo-2,5-difluorobenzene