Belizatinib
Based on 1 publication(s) in Google Scholar
Belizatinib (TSR-011) is an orally active, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7 nM for wild-type recombinant ALK kinase.
For research use only. We do not sell to patients.
- Purity: 99.62%
- CAS No.: 1357920-84-3
- Formula: C33H44FN5O3
- Molecular Weight:577.73
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Belizatinib
More
Biological Activity
|
TrkA |
TrkB |
TrkC |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
231 nM
Compound: 36
|
Inhibition of INSR expressed in CHO cells assessed as inhibition of receptor phosphorylation pre-incubated before insulin stimulation by Meso-Scale Discovery pY-IR assay
Inhibition of INSR expressed in CHO cells assessed as inhibition of receptor phosphorylation pre-incubated before insulin stimulation by Meso-Scale Discovery pY-IR assay
|
[PMID: 22734674] |
Belizatinib (TSR-011) has antitumour activity.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 1357920-84-3
-
Appearance Solid
-
Molecular Weight 577.73
-
Formula C33H44FN5O3
-
Color White to off-white
-
SMILES
O=C(NC1=NC2=CC=C(CN3CCC(C(C)(O)C)CC3)C=C2N1[C@H]4CC[C@@H](C(NC(C)C)=O)CC4)C5=CC=C(F)C=C5
-
Synonyms
TSR-011
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
J Pharm Biomed Anal
Belizatinib: Novel reactive intermediates and bioactivation pathways characterized by LC-MS/MS. [Abstract]2019 Jul 15:171:132-147. PMID: 30999224
Solvent & Solubility
DMSO : ≥ 300 mg/mL (519.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (272 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7309 mL | 8.6546 mL | 17.3091 mL | 43.2728 mL |
| 5 mM | 0.3462 mL | 1.7309 mL | 3.4618 mL | 8.6546 mL | |
| 10 mM | 0.1731 mL | 0.8655 mL | 1.7309 mL | 4.3273 mL | |
| 15 mM | 0.1154 mL | 0.5770 mL | 1.1539 mL | 2.8849 mL | |
| 20 mM | 0.0865 mL | 0.4327 mL | 0.8655 mL | 2.1636 mL | |
| 25 mM | 0.0692 mL | 0.3462 mL | 0.6924 mL | 1.7309 mL | |
| 30 mM | 0.0577 mL | 0.2885 mL | 0.5770 mL | 1.4424 mL | |
| 40 mM | 0.0433 mL | 0.2164 mL | 0.4327 mL | 1.0818 mL | |
| 50 mM | 0.0346 mL | 0.1731 mL | 0.3462 mL | 0.8655 mL | |
| 60 mM | 0.0288 mL | 0.1442 mL | 0.2885 mL | 0.7212 mL | |
| 80 mM | 0.0216 mL | 0.1082 mL | 0.2164 mL | 0.5409 mL | |
| 100 mM | 0.0173 mL | 0.0865 mL | 0.1731 mL | 0.4327 mL |