PeptideDB

DD-03-156 ((S,R,S)-AHPC-Me-PEG2-dabrafenib) 2769753-69-5

DD-03-156 ((S,R,S)-AHPC-Me-PEG2-dabrafenib) 2769753-69-5

CAS No.: 2769753-69-5

DD-03-156 is a potent and specific degrader of CDK17 and LIMK2. The selectivity and potency of DD-03-156 are very good,
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DD-03-156 is a potent and specific degrader of CDK17 and LIMK2. The selectivity and potency of DD-03-156 are very good, providing an advanced starting point for the development of chemical probes to degrade CDK17. DD-03-156 is a potent and specific degrader of CDK17 and LIMK2. The selectivity and potency of DD-03-156 are very good, providing an advanced starting point for the development of chemical probes to degrade CDK17.

Physicochemical Properties


Molecular Formula C53H62F3N9O8S3
Molecular Weight 1106.30509901047
CAS # 2769753-69-5
PubChem CID 163196237
Appearance White to off-white solid powder
Hydrogen Bond Donor Count 5
Hydrogen Bond Acceptor Count 19
Rotatable Bond Count 23
Heavy Atom Count 76
Complexity 1990
Defined Atom Stereocenter Count 4
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 (e.g. under nitrogen), 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 LIMK2
References

[1]. Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development. Cell. 2020;183(6):1714-1731.e10.


Solubility Data


Solubility (In Vitro) DMSO : 200 mg/mL (180.78 mM)
H2O : < 0.1 mg/mL
Solubility (In Vivo) Solubility in Formulation 1: 5 mg/mL (4.52 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 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: 5 mg/mL (4.52 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 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: ≥ 5 mg/mL (4.52 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 50.0 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.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.9039 mL 4.5195 mL 9.0391 mL
5 mM 0.1808 mL 0.9039 mL 1.8078 mL
10 mM 0.0904 mL 0.4520 mL 0.9039 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.