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Dasatinib analog-1 1174416-41-1

Dasatinib analog-1 1174416-41-1

CAS No.: 1174416-41-1

Dasatinib Analog-1 inhibits CYP3A4 activity with a Ki value of 5.4 μM. Dasatinib Analog-1 blocks the formation of gluta
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Dasatinib Analog-1 inhibits CYP3A4 activity with a Ki value of 5.4 μM. Dasatinib Analog-1 blocks the formation of glutathione adducts.

Physicochemical Properties


CAS # 1174416-41-1
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

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


References

[1].Characterization of dasatinib and its structural analogs as CYP3A4 mechanism-based inactivators and the proposed bioactivation pathways. Drug Metab Dispos. 2009, 37, 6.


Solubility Data


Solubility (In Vitro) DMSO :~25 mg/mL (~49.41 mM; ultrasonic and warming and adjust pH to 2 with 1M HCl and heat to 80°C)
Solubility (In Vivo) Solubility in Formulation 1: 2.5 mg/mL (4.94 mM) 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; with ultrasonication.
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 and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up 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 (4.94 mM) 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; with ultrasonication.
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 and add it to 900 μL of 20% SBE-β-CD saline solution and mix well.
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 (4.94 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication.
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 and add it to 900 μL corn oil and mix well.

 (Please use freshly prepared in vivo formulations for optimal results.)