AdipoGen Life Sciences

BBT594

Product Code:
 
SYN-1225
Product Group:
 
Inhibitors and Activators
Regulatory Status:
 
RUO
Storage:
 
+4°C
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Chemical Structure
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Chemical Structure

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Further Information

Alternate Names/Synonyms:
BBT-594
Appearance:
Solid.
CAS:
882405-89-2
EClass:
32160000
Form (Short):
liquid
InChi:
InChI=1S/C28H30F3N7O3/c1-18(39)34-25-15-26(33-17-32-25)41-22-5-6-24-19(13-22)7-8-38(24)27(40)35-21-4-3-20(23(14-21)28(29,30)31)16-37-11-9-36(2)10-12-37/h3-6,13-15,17H,7-12,16H2,1-2H3,(H,35,40)(H,32,33,34,39)
InChiKey:
VQLNKQZLPGLOSI-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 882405-89-2. Formula: C28H30F3N7O3. MW: 569.6. 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.
Molecular Formula:
C28H30F3N7O3
Molecular Weight:
569.6
Package Type:
Plastic Vial
Product 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.
Purity:
>95%
Solubility Chemicals:
Soluble in DMSO.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.

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)