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Purity: ≥98%
BSJ-03-123 is a novel, potent cyclin-dependent kinase 6 (CDK6)-selective small-molecule degrader (PROTAC: proteolysis targeting chimera). It is a phthalimide-based degrader that exploits protein-interface determinants to achieve proteome-wide selectivity for the degradation of cyclin-dependent kinase 6 (CDK6). Pharmacologic CDK6 degradation targets a selective dependency of acute myeloid leukemia cells, and transcriptomics and phosphoproteomics profiling of acute degradation of CDK6 enabled dynamic mapping of its immediate role in coordinating signaling and transcription.
| ln Vitro |
BSJ-03-123 (BSJ) induces G1 cell cycle arrest without appreciably boosting apoptosis, hence exerting strong antiproliferative effects in CDK6-dependent AML cell lines [1].
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| References |
[1]. Brand M, et al. Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML. Cell Chem Biol. 2019 Feb 21;26(2):300-306.e9.
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| Molecular Formula |
C47H56N10O11
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|---|---|
| Molecular Weight |
937.007950782776
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| CAS # |
2361493-16-3
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| Related CAS # |
BSJ-03-123 HCl;2361493-16-3;
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| SMILES |
O=C(NCCOCCOCCOCCN1CCN(C2=CC=C(NC3=CC4=C(C=N3)C(C)=C(C(C)=O)C(N4C5CCCC5)=O)N=C2)CC1)COC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O
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| InChi Key |
PHXAASMYZCBYHV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C48H57N9O11/c1-30-35-28-51-40(26-37(35)56(32-6-3-4-7-32)47(63)43(30)31(2)58)52-39-12-10-33(27-50-39)55-17-15-54(16-18-55)19-21-66-23-25-67-24-22-65-20-14-49-42(60)29-68-38-9-5-8-34-44(38)48(64)57(46(34)62)36-11-13-41(59)53-45(36)61/h5,8-10,12,26-28,32,36H,3-4,6-7,11,13-25,29H2,1-2H3,(H,49,60)(H,50,51,52)(H,53,59,61)
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| Chemical Name |
N-(2-(2-(2-(2-(4-(6-((3-acetyl-1-cyclopentyl-4-methyl-2-oxo-1,2-dihydro-1,6-naphthyridin-7-yl)amino)pyridin-3-yl)piperazin-1-yl)ethoxy)ethoxy)ethoxy)ethyl)-2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamide
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| Synonyms |
BSJ-03123; BSJ03123; BSJ 03123; BSJ-03-123; BSJ03-123; BSJ 03-123
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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 : ~100 mg/mL (~106.72 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.67 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 (2.67 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0672 mL | 5.3361 mL | 10.6722 mL | |
| 5 mM | 0.2134 mL | 1.0672 mL | 2.1344 mL | |
| 10 mM | 0.1067 mL | 0.5336 mL | 1.0672 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.
Cell Chem Biol.2019 Feb 21;26(2):300-306.e9. |
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