Size | Price | Stock | Qty |
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1mg |
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5mg |
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Other Sizes |
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Purity: ≥98%
BI-3663 is a novel, potent, functional and highly selective PTK2/FAK degrader based on PROTAC (proteolysis-targeting chimeras) technology, utilizing VHL (von Hippel-Lindau) and cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. Focal adhesion tyrosine kinase (PTK2) is often overexpressed in human hepatocellular carcinoma (HCC), and several reports have linked PTK2 depletion and/or pharmacological inhibition to reduced tumorigenicity. However, the clinical relevance of targeting PTK2 still remains to be proven. BI-3663 (cereblon-based) degrades PTK2 with a median DC50 of 30 nM to >80% across a panel of 11 HCC cell lines. Despite effective PTK2 degradation, these compounds did not phenocopy the reported antiproliferative effects of PTK2 depletion in any of the cell lines tested.
ln Vitro |
In Hep3B2.1-7 cells and A549 cells, BI-3663 can efficiently degrade PTK2, with pDC50s of 7.6 and 7.9, respectively [1].
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References |
[1]. Popow J, et al. Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions. J Med Chem. 2019 Mar 14;62(5):2508-2520.
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Molecular Formula |
C44H42F3N7O12
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Molecular Weight |
917.839201450348
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CAS # |
2341740-84-7
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SMILES |
FC(C1=CN=C(NC2C=CC(C(NCCOCCOCCOCCC(NC3=CC=CC4C(N(C(C=43)=O)C3C(NC(CC3)=O)=O)=O)=O)=O)=CC=2OC)N=C1OC1=CC=CC2=C1C(CC2)=O)(F)F
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Synonyms |
BI-3663
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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 : ~300 mg/mL (~326.85 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 7.5 mg/mL (8.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 75.0 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.0895 mL | 5.4476 mL | 10.8951 mL | |
5 mM | 0.2179 mL | 1.0895 mL | 2.1790 mL | |
10 mM | 0.1090 mL | 0.5448 mL | 1.0895 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.