Specifications
- Purity
- ≥98% (HPLC)
- Appearance
- White to yellow solid
- Identity
- 1H-NMR
Properties
- Solvents
- DMSO, ethanol (sligthly), water (insoluble)
Category: API's & Intermediates
Brigitanib acts as a tyrosine kinase inhibitor with activity against multiple kinases including ALK, ROS1, insulin-like growth factor 1 receptor and against EGFR deletions and point mutations. It acts by inhibiting ALK phosphorylation and the activation of downstream signaling proteins. It is a highly potent and selective inhibitor of anaplastic lymphoma kinase (ALK). Blocks ALK activity and reduces growth in neuroblastoma cells, mouse xenograft, and Drosophila model systems harboring constitutively active ALK variants. It is potentially useful for the treatment of non-small cell lung cancer (NSCLC). Can be used in combination with anti-EGFR drugs to overcome EGFR mutation resistance.
Synonyms | AP26113, 5-Chloro-N4-[2-(dimethylphosphinyl)phenyl]-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-2,4-pyrimidinediamine |
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Purity | ≥98% (HPLC) |
Appearance | White to yellow solid |
CAS-Number | 1197953-54-0 |
Molecular Formula | C29H39ClN7O2P |
Molecular Weight | 584.09 |
Identity | 1H-NMR |
Solvents | DMSO, ethanol (sligthly), water (insoluble) |
Smiles | CN1CCN(C2CCN(C3=CC=C(NC4=NC(NC5=CC=CC=C5P(C)(C)=O)=C(Cl)C=N4)C(OC)=C3)CC2)CC1 |
InChi Key | AILRADAXUVEEIR-UHFFFAOYSA-N |
Shipping | AMBIENT |
Short Term Storage | +4°C |
Long Term Storage | -20°C |
Handling Advice | Protect from light and moisture. |
Use / Stability | Stable for at least 2 years after receipt when stored at -20°C. |
Transportation | Not dangerous goods |
References | (1) R. Katayama, et al., PNAS 108, 7535 (2011), (2) M. Ceccon, et al., Mol. Cancer Res. 11, 122 (2013), (3) J.T. Siaw, et al., Oncotarget 7, 29011 (2016), (4) W.S. Huang, et al., J. Med. Chem. 59, 4948 (2016), (5) S. Zhang, et al., Clin. Cancer Res. 22, 5527 (2016), (6) K. Uchibori, et al., Nat. Commun. 8, 14768 (2017), (7) L. Mezquita & D. Planchard, Cancer Manag. Res. 10, 123 (2018), (8) S.A. Spencer, et al., Ann. Pharmacother. 53, 621 (2019) |
Quantity | 5 mg, Bulk |