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SynKinase
BBT594
CHF 0.00
In stock
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| Product Details | |
|---|---|
| Synonyms | BBT-594 |
| Product Type | Chemical |
| Properties | |
| Formula | C28H30F3N7O3 |
| MW | 569.6 |
| CAS | 882405-89-2 |
| Purity Chemicals | ≥95% |
| Appearance | Solid. |
| Solubility | Soluble in DMSO. |
| Declaration | Manufactured by SynKinase. |
| Other Product Data |
Target: JAK2 | 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 | VQLNKQZLPGLOSI-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
BBT594 (NVP-BBT594) is a potent and selective inhibitor of RET and JAK2. BBT594 impairs "glial-derived neurotrophic factor" (GDNF)-RET signaling and GDNF-dependent growth in specific in vitro models. Direct inhibition of GDNF-RET signaling by BBT594 in ER+ breast cancer cells enhances the sensitivity to aromatase inhibitor (AI) treatment and reverts AI resistance. In murine models, the IC50 of BBT594 on JAK2 inhibition varies between 8nM - 29nM, depending on the cell model and abundant JAK2 mutations.
Product References
- Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent: R. Andraos, et al.; Cancer Discov. 2, 512 (2012)
- GDNF-RET signaling in ER-positive breast cancers is a key determinant of response and resistance to aromatase inhibitors: A. Morandi, et al.; Cancer Res. 73, 3783 (2013)
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