[CAS NO. 882405-89-2] BBT594
PRODUCTS SPECIFICATIONS [882405-89-2]
DESCRIPTION [882405-89-2]
Overview
| MDL | MFCD30533519 |
|---|---|
| Molecular Weight | 569.58 |
| Molecular Formula | C28H30F3N7O3 |
| SMILES | O=C(N1CCC2=C1C=CC(OC3=NC=NC(NC(C)=O)=C3)=C2)NC4=CC=C(CN5CCN(C)CC5)C(C(F)(F)F)=C4 |
1 Publications Citing Use of MCE
Summary
BBT594 is a potent receptor tyrosine kinase RET inhibitor , used for cancer treatment.
In Vitro
NVP-BBT594 blocks the GDNF-mediated enhancement of MCF7-LTED cell viability in 2D culture and 3D colony formation. The addition of 10 pM E2, to mimic the E2 level in post-menopausal patients that have relapsed on AI treatment and ceased AI therapy, increases 3D colony formation of both MCF7 and MCF7-LTED cells, and this effect is efficiently reverted by NVP-BBT594. Parental T47D cells cultured in presence of low level E2, GFRα1/GDNF stimulation results in increased 3D colony formation, which is significantly reverted by NVP-BBT594. NVP-BBT594 targets GDNF-RET signaling and sensitizes MCF7-2A cells to letrozole treatment. NVP-BBT594 impairs GDNF-mediated RET downstream signaling and significantly enhances the antiproliferative effects of letrozole [1] . NVP-BBT594 shows the highest suppression of GDNF-induced RET signaling, as assessed by RET, ERK1/2, AKT and ER phosphorylation. NVP-AST487 and NVP-BBT594 have comparable RET inhibitory activity in wild-type MCF7 cells [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 33 mg/mL ( 57.94 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7557 mL | 8.7784 mL | 17.5568 mL |
| 5 mM | 0.3511 mL | 1.7557 mL | 3.5114 mL |
| 10 mM | 0.1756 mL | 0.8778 mL | 1.7557 mL |
References
- [1] Morandi A, et al. GDNF-RET signaling in ER-positive breast cancers is a key determinant of response and resistance to aromatase inhibitors. Cancer Res. 2013 Jun 15;73(12):3783-95
- [2] Andreucci E, et al. Targeting the receptor tyrosine kinase RET in combination with aromatase inhibitors in ER positive breast cancer xenografts. Oncotarget. 2016 Sep 2. doi: 10.18632/oncotarget.11826. [Epub ahead of print]