Physicochemical Properties
| CAS # | 2785404-83-1 |
| Appearance | Off-white to light yellow solid powder |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| Targets | HDAC6 19.4 nM (ID50) HDAC6 4.54 nM (IC50) HDAC1 0.647 μM (IC50) Cereblon |
| ln Vitro | HDAC6 degrader-3 (Compound B4) demonstrates effective HDAC6 degradation and hyperacetylation of α-tubulin over a 24-hour period at 100-1000 nM [1]. Leukemia cell lines (697, HL-60, KASUMI-1, MV4-11, REH, THP-1, SKNO-1, MOLM-13) were treated with HDAC6 degrader-3 (0.5-50 μM; 72 hours) [1]. |
| Cell Assay |
Western Blot Analysis[1] Cell Types: U266 multiple myeloma cell line Tested Concentrations: 100 nM and 1000 nM Incubation Duration: 24 h Experimental Results: Demonstrated potent HDAC6 degradation as well as hyperacetylation of α-tubulin. |
| References |
[1]. Solid-Phase Synthesis of Cereblon-Recruiting Selective Histone Deacetylase 6 Degraders (HDAC6 PROTACs) with Antileukemic Activity. J Med Chem. 2022 Dec 22;65(24):16860-16878. |
Solubility Data
| Solubility (In Vitro) | DMSO : 100 mg/mL (113.15 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.83 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 (2.83 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. Solubility in Formulation 3: ≥ 2.5 mg/mL (2.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |