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SynKinase
BGG463
CHF 0.00
In stock
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| Product Details | |
|---|---|
| Synonyms | BGG-463 |
| Product Type | Chemical |
| Properties | |
| Formula | C30H29F3N6O3 |
| MW | 578.6 |
| CAS | 890129-26-7 |
| Purity Chemicals | ≥95% (HPLC) |
| Appearance | Solid. |
| Solubility | Soluble in DMSO. |
| Declaration | Manufactured by SynKinase. |
| Other Product Data |
Target: Src - Abl | Kinase Group: PTK | Substrate: Tyrosine Click here for Original Manufacturer Product Datasheet Our product description may differ slightly from the original manufacturers product datasheet. |
| InChi Key | MZZJNOOADWVFPD-UHFFFAOYSA-N |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
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.
Product References
Rational design of T315I BCR-Abl inhibitors for the treatment of drug-resistant chronic myelogenous leukemia (CML): BGG463: P.W. Manley, et al.; Chimia (Aarau) 62, 579 (2008)