LY-3381916

Catalog No.S8919 Batch:S891901

Print

Technical Data

Formula
C23H25FN2O3
Molecular Weight 396.45 CAS No. 2166616-75-5
Solubility (25°C)* In vitro DMSO 79 mg/mL (199.26 mM)
Ethanol 20 mg/mL (50.44 mM)
Water Insoluble
In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 3.95mg/ml (9.96mM) Taking the 1 mL working solution as an example, add 50 μL of 79 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution
5% DMSO 95% Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 0.395mg/ml (1.00mM) Taking the 1 mL working solution as an example, add 50 μL of 7.9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description LY-3381916 (IDO1-IN-5) is a brain-penetrating, potent and selective Indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor. This compound exhibits anti-tumour activity.
Targets
IDO1
In vitro

LY3381916 binds to newly synthesised apo-IDO1 lacking haem, but does not inhibit mature haem-bound IDO1. Protein x-ray crystallography confirms that this compound binds to apo-IDO1 where it occupies the haem-binding pocket of IDO1. Modelling of the pre-clinical PK/PD relationship suggests QD dosing of this chemical will maintain greater than 90% inhibition over 24 hours. In addition, due to the favourable properties of the drug, significant central nervous system (CNS) penetration has been measured for this compound.

Protocol (from reference)

References

  • https://cancerres.aacrjournals.org/content/78/13_Supplement/5245#

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.