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Purity: ≥98%
BBT-594 (also known as NVP-BBT594) is a novel, potent and selective receptor tyrosine kinase RET inhibitor used for cancer treatment. BBT594 inhibits MCF7-LTED cell growth that is dependent on GDNF and GDNF-RET signaling. By focusing on GDNF-RET signaling, it makes MCF7-2A cells more susceptible to letrozole treatment. As a logical therapeutic target, GDNF-RET signaling may help prevent or postpone the emergence of AI resistance in breast cancer.
| ln Vitro |
NVP-BBT594 inhibits the growth of MCF7-LTED cell viability in 2D culture and 3D colony formation, which is mediated by GDNF. Both MCF7 and MCF7-LTED cells form more 3D colonies when 10 pM E2, which is added to replicate the E2 level in post-menopausal patients who have relapsed on AI therapy and stopped AI therapy, is added. NVP-BBT594 effectively reverses this effect. NVP-BBT594 significantly reverses the increased formation of 3D colonies in parental T47D cells cultured in the presence of low level E2, GFRα1/GDNF stimulation. MCF7-2A cells become more susceptible to letrozole treatment when NVP-BBT594 targets GDNF-RET signaling. Letrozole's antiproliferative effects are markedly enhanced by NVP-BBT594, which also inhibits GDNF-mediated RET downstream signaling[1]. According to phosphorylation of RET, ERK1/2, AKT, and ER, NVP-BBT594 exhibits the strongest suppression of GDNF-induced RET signaling. Comparable RET inhibitory activity has been observed for NVP-AST487 and NVP-BBT594 in wild-type MCF7 cells [2].
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| References |
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| Molecular Formula |
C28H30F3N7O3
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|---|---|
| Molecular Weight |
569.5781
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| Exact Mass |
569.236
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| Elemental Analysis |
C, 59.04; H, 5.31; F, 10.01; N, 17.21; O, 8.43
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| CAS # |
882405-89-2
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| Related CAS # |
882405-89-2
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| PubChem CID |
59596344
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| Appearance |
White to khaki solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
723.9±70.0 °C at 760 mmHg
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| Flash Point |
391.6±35.7 °C
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| Vapour Pressure |
0.0±2.5 mmHg at 25°C
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| Index of Refraction |
1.640
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| LogP |
3.28
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
41
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| Complexity |
904
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(N1CCC2C1=CC=C(C=2)OC1C=C(NC(C)=O)N=CN=1)NC1C=C(C(F)(F)F)C(CN2CCN(C)CC2)=CC=1
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| InChi Key |
VQLNKQZLPGLOSI-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
5-(6-acetamidopyrimidin-4-yl)oxy-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-2,3-dihydroindole-1-carboxamide
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| Synonyms |
BBT-594; BBT-594; BBT-594; NVP BBT594; NVP-BBT594; NVP BBT-594
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 33 mg/mL (~57.9 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.39 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.39 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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