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  • DC Chemicals Limited
  • China
  • Product Name: BBT594
  • Price: $350.0/10mg $650.0/25mg $1500.0/100mg
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

882405-89-2

882405-89-2 structure
882405-89-2 structure
  • Name: BBT594
  • Chemical Name: BBT594
  • CAS Number: 882405-89-2
  • Molecular Formula: C28H30F3N7O3
  • Molecular Weight: 569.578
  • Catalog: Research Areas Cancer
  • Create Date: 2018-03-08 01:45:39
  • Modify Date: 2024-01-02 13:08:16
  • BBT594 is a potent receptor tyrosine kinase RET inhibitor, used for cancer treatment.

Name BBT594
Synonyms 1H-Indole-1-carboximidic acid, 2,3-dihydro-5-[[6-[[(1E)-1-hydroxyethylidene]amino]-4-pyrimidinyl]oxy]-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-
NVP-BBT594
5-({6-[(E)-(1-Hydroxyethylidene)amino]-4-pyrimidinyl}oxy)-N-{4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl}-1-indolinecarboximidic acid
Description BBT594 is a potent receptor tyrosine kinase RET inhibitor, used for cancer treatment.
Related Catalog
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].
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]

Density 1.4±0.1 g/cm3
Boiling Point 723.9±70.0 °C at 760 mmHg
Molecular Formula C28H30F3N7O3
Molecular Weight 569.578
Flash Point 391.6±35.7 °C
Exact Mass 569.236206
LogP 3.28
Vapour Pressure 0.0±2.5 mmHg at 25°C
Index of Refraction 1.640
Storage condition 2-8℃