Brigatinib
| Code | Size | Price |
|---|
| CDX-B0374-M005 | 5 mg | £84.00 |
Quantity:
| CDX-B0374-M025 | 25 mg | £304.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
AMBIENT
Storage:
Short Term: +4°C, Long Term: -20°C
Documents
Further Information
Alternate Names/Synonyms:
AP26113; 5-Chloro-N4-[2-(dimethylphosphinyl)phenyl]-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-2,4-pyrimidinediamine
Appearance:
White to yellow solid.
CAS:
1197953-54-0
EClass:
32160000
Form (Short):
liquid
Handling Advice:
Protect from light and moisture.
InChi:
InChI=1S/C29H39ClN7O2P/c1-35-15-17-37(18-16-35)21-11-13-36(14-12-21)22-9-10-24(26(19-22)39-2)33-29-31-20-23(30)28(34-29)32-25-7-5-6-8-27(25)40(3,4)38/h5-10,19-21H,11-18H2,1-4H3,(H2,31,32,33,34)
InChiKey:
AILRADAXUVEEIR-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 1197953-54-0. Formula: C29H39ClN7O2P. MW: 584.09. Synthetic. 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.
MDL:
MFCD29472221
Molecular Formula:
C29H39ClN7O2P
Molecular Weight:
584.09
Package Type:
Vial
Product Description:
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.
Purity:
>98% (HPLC)
SMILES:
CN1CCN(C2CCN(C3=CC=C(NC4=NC(NC5=CC=CC=C5P(C)(C)=O)=C(Cl)C=N4)C(OC)=C3)CC2)CC1
Solubility Chemicals:
Soluble in DMSO. Sligthly soluble in ethanol. Insoluble in water.
Source / Host:
Synthetic
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
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)