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;Larotrectinib sulphate;ARRY-470, Larotrectinib
- CBNumber:
- CB93067010
- Molecular Formula:
- C21H24F2N6O6S
- Molecular Weight:
- 526.52
- MDL Number:
- MFCD29472286
- MOL File:
- 1223405-08-0.mol
| Product description | Number | Pack Size | Price |
| LarotrectinibSulfate | L175933 | 100mg | $55 |
| Larotrectinibsulfate 99.69% | CS-5314 | 5mg | $60 |
| LOXO-101 | B6176 | 5mg | $68 |
| Larotrectinib sulphate | BL161518 | 10mg | $90 |
| Larotrectinibsulfate 99.69% | CS-5314 | 10mg | $100 |
| More product size | |||
| 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 |
| 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| |
| NCI Dictionary of Cancer Terms | larotrectinib sulfate |
| FDA UNII | RDF76R62ID |
| NCI Drug Dictionary | larotrectinib sulfate |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
Larotrectinib Sulfate price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| TRC | L175933 | LarotrectinibSulfate | 1223405-08-0 | 100mg | $55 | 2021-12-16 | Buy |
| ChemScene | CS-5314 | Larotrectinibsulfate 99.69% | 1223405-08-0 | 5mg | $60 | 2021-12-16 | Buy |
| ApexBio Technology | B6176 | LOXO-101 | 1223405-08-0 | 5mg | $68 | 2021-12-16 | Buy |
| Biosynth Carbosynth | BL161518 | Larotrectinib sulphate | 1223405-08-0 | 10mg | $90 | 2021-12-16 | Buy |
| ChemScene | CS-5314 | Larotrectinibsulfate 99.69% | 1223405-08-0 | 10mg | $100 | 2021-12-16 | Buy |
Larotrectinib Sulfate Chemical Properties,Uses,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 oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).
Uses
Larotrectinib Sulfate is a potent and selective oral ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).
Mechanism of action
Larotrectinib sulfate functions as an inhibitor of TRKs including TRKA, B, and C. In in vitro and in vivo tumor models, larotrectinib demonstrated anti-tumor activity in cells with constitutive activation of TRK proteins resulting from gene fusions, deletion of a protein regulatory domain, or in cells with TRK protein overexpression. Larotrectinib had minimal activity in cell lines with point mutations in the TRKA kinase domain, including the clinically identified acquired resistance mutation, G595R. Point mutations in the TRKC kinase domain with clinically identified acquired resistance to larotrectinib include G623R, G696A, and F617L.
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 (Larotrectinib Sulfate) 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 (Larotrectinib Sulfate) 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
1of2
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Zhengzhou Anhuida Chemical Co., Ltd | +8615903659408 | admin@ahdchem.com | China | 286 | 58 |
| Beijing Hope Pharmaceutical Co., Ltd. | +86-010-67886402 +8613611125266 | market@hopelife.cn | China | 72 | 58 |
| BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. | +86-18600796368 | sales@sjar-tech.com | China | 504 | 58 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| Ningbo Nuobai Pharmaceutical Co., Ltd. | 18758416982 | Fisheryu@nbpharm.com | China | 13 | 58 |
| Shenzhen Nexconn Pharmatechs Ltd | +86-755-89396905 +86-15013857715 | admin@nexconn.com | China | 10405 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19552 | 58 |
| Shenzhen Excellent Biotech Co., Ltd. | 13480692018 | ramyan@ex-biotech.com | CHINA | 954 | 58 |
| career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29795 | 58 |
| Shaanxi Dideu Medichem Co. Ltd | +86-29-87569266 +86-17392581500 | 1015@dideu.com | China | 3987 | 58 |
View Lastest Price from Larotrectinib Sulfate manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2026-01-13 | Larotrectinib sulfate
1223405-08-0
|
US $52.00-133.00 / mg | 98.62% | 10g | TargetMol Chemicals Inc. | ||
 |
2025-09-11 | Larotrectinib Sulfate
1223405-08-0
|
US $0.00 / g | 1g | More Than 99% | 100kg/Month | BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. | |
 |
2025-09-11 | Larotrectinib Sulfate.
1223405-08-0
|
US $0.00 / g | 1g | More Than 99% | 100kg/Month | BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. |
-
- Larotrectinib sulfate
1223405-08-0
- US $52.00-133.00 / mg
- 98.62%
- TargetMol Chemicals Inc.
-
- Larotrectinib Sulfate
1223405-08-0
- US $0.00 / g
- More Than 99%
- BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
-
- Larotrectinib Sulfate.
1223405-08-0
- US $0.00 / g
- More Than 99%
- BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
