Bulk Inquiry
Brigatinib
- AP 26113 - Alunbrig
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C29H39ClN7O2P
- MW: 584.09
Description
Brigatinib is a potent and selective inhibitor of ALK (IC50 value of 0.6 nM), capable of overcoming mechanisms of resistance associated with crizotinib (Axon 1660). Besides inhibition of ALK, FLT3 and ROS1 were also potently inhibited. Brigatinib was highly active against both sensitive and resistant H3122 cells, decreasing cell growth, suppressing ALK phosphorylation, and inducing apoptosis.
More Information
| Parent CAS No. | 1197953-54-0 |
|---|---|
| Chemical Name | 5-Chloro-N4-(2-(dimethylphosphoryl)phenyl)-N2-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)pyrimidine-2,4-diamine |
| SMILES | C1C(OC)=C(NC2N=CC(Cl)=C(NC3C(P(C)(C)=O)=CC=CC=3)N=2)C=CC=1N1CCC(N2CCN(C)CC2)CC1 |
| MFCD | N.A. |
| 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 |
| CID | 68165256 |
| Short Description | ALK inhibitor |
References
- R Katayama et al. Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc Natl Acad Sci U S A. 2011 May 3;108(18):7535-40.
- WS Huang et al. Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem. 2016 May 26;59(10):4948-64.
- S Zhang et al. The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models. Clin Cancer Res. 2016 Nov 15;22(22):5527-5538.
Related Products
| AXON ID | NAME | FROM PRICE |
|---|---|---|
| 1416 | NVP-TAE684 |
From $55.00 |
| 1660 | Crizotinib |
From $88.00 |
| 1884 | Alectinib |
From $77.00 |
| 2005 | ASP 3026 |
From $88.00 |
| 2153 | AZD3463 |
From $115.50 |
| 2224 | LDK 378 |
From $104.50 |
| 2267 | GSK 1838705A |
From $121.00 |
| 2294 | KRCA 0008 |
From $104.50 |
| 2600 | PF 06463922 |
From $115.50 |
| 3931 | CEP-28122 |
From Inquiry |
| 3969 | Crenolanib |
From Inquiry |
| 3973 | XL-228 |
From Inquiry |
| 3998 | MGCD516 |
From Inquiry |
| 4038 | CEP-37440 hydrochloride |
From Inquiry |
Other Categories
Are you sure you would like to remove this item from the shopping cart?
This item is a part of the approved quote. Removing it will remove all quote items from the cart.