Cas No.: | 890129-26-7 |
Synonyms: | BGG 463,BGG-463 |
SMILES: | CC(=O)NC1=CC(=NC=N1)OC2=CC3=C(C=C2)C(=CC=C3)C(=O)NC4=CC(=C(C=C4)CN5CCN(CC5)C)C(F)(F)F |
Formula: | C30H29F3N6O3 |
M.Wt: | 578.58 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | BGG463 (NVP-BGG463) was generated by a rational ‘hybrid design’ approach. Like Imatinib, BGG463 disrupts the assembly of the hydrophobic spine, a characteristic feature of the active state of several kinases, thereby locking the kinase in an inactive ‘DFG-out’ conformation. BGG463 can inhibit c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants with a 50% inhibitory concentration (IC50) of 0.25 μM, 0.09 μM and 0.590 μM, respectively. |
Target: | CDK2 |
References: | [1]. Alexander LT, et al. Type II Inhibitors Targeting CDK2. ACS Chem Biol. 2015 Sep 18;10(9):2116-25. |