Loading...

Skip to main content

Call us on + 1 (800) 604-9114 for more information about our products

Looking for specific datasheet Manual/COA/MSDS?
Request a Manual/COA/MSDS

Interested to get a quote about our products?
Request a Quote

Structure

BMS-986165, inhibitor

BMS-986165

Purity
98.00%
Synonyms
BMS-986165; inhibitor
Ordering
For Research Use Only!
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
DMSO: 32.5mg/ml (76.39mM) Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C20H19D3N8O3
SMILES
[2H]C([2H])([2H])NC(=O)C1=NN=C(NC(=O)C2CC2)C=C1NC1=CC=CC(C2=NN(C)C=N2)=C1OC
CAS Number
1609392-27-9
Target & IC50
Tyk2 JH2: ic50 0.2nM
JAK1 JH2: ic50 1nM
In Vitro
BMS-986165 as a high affinity JH2 ligand and potent allosteric inhibitor of TYK2. In addition to unprecedented JAK isoform and kinome selectivity, BMS-986165 shows excellent pharmacokinetic properties with minimal profiling liabilities and is efficacious in several murine models of autoimmune disease. On the basis of these findings, BMS-986165 appears differentiated from all other reported JAK inhibitors and has been advanced as the first pseudokinase-directed therapeutic in clinical development as an oral treatment, for autoimmune diseases[1].
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

Structure

Structure
Related Product Information for BMS-986165, inhibitor
BMS-986165 inhibits IL-12/23 and type I IFN pathways[1][2]. BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment,of autoimmune diseases. Which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain.
References
Wrobleski ST, et al. Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the treatment,of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165. J Med Chem. 2019 Jul 18.
Wrobleski ST, et al. Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the treatment,of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165. J Med Chem. 2019 Jul 18.
Catlett I, et al. SAT0226 A first-in-human, study of BMS-986165, a selective, potent, allosteric small molecule inhibitor of tyrosine kinase Annals of the Rheumatic Diseases 2017;76:859.
Catlett I, et al. SAT0226 A first-in-human, study of BMS-986165, a selective, potent, allosteric small molecule inhibitor of tyrosine kinase 2. Annals of the Rheumatic Diseases 2017;76:859.

Similar Products

Product Notes

The BMS-986165 (Catalog #AAA5754633) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "BMS-986165, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.

Precautions

All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.

Disclaimer

Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.

Item has been added to Shopping Cart

If you are ready to order, navigate to Shopping Cart and get ready to checkout.

Looking for a specific manual?
Request a Manual

Request more Information

Please complete the form below and a representative will contact you as soon as possible.

Request a Manual

Please complete the form below and a representative will contact you as soon as possible.

Request a Quote

Please complete the form below and a representative will contact you as soon as possible.