1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
    Immunology/Inflammation
  2. JAK
    Interleukin Related
  3. BMS-986165

BMS-986165 

Cat. No.: HY-117287 Purity: 99.76%
Handling Instructions

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=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. BMS-986165 inhibits IL-12/23 and type I IFN pathways.

For research use only. We do not sell to patients.

BMS-986165 Chemical Structure

BMS-986165 Chemical Structure

CAS No. : 1609392-27-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 605 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. BMS-986165 inhibits IL-12/23 and type I IFN pathways[1][2].

IC50 & Target[1]

Tyk2 JH2

0.2 nM (IC50)

JAK1 JH2

1 nM (IC50)

In Vitro

BMS-986165 is differentiated from previous JAK inhibitors due its unique ability to selectively bind to the pseudokinase (JH2) domain of TYK2 and inhibit its function through an allosteric mechanism[1].
BMS-986165 maintains excellent potency in human and mouse whole blood (IC50s=13 and 100 nM, respectively) and shows no significant hERG inhibition in the flux assay (IC50>80 μM)[1].

Molecular Weight

425.46

Formula

C₂₀H₁₉D₃N₈O₃

CAS No.

1609392-27-9

SMILES

O=C(C1=NN=C(NC(C2CC2)=O)C=C1NC3=CC=CC(C4=NN(C)C=N4)=C3OC)NC([2H])([2H])[2H]

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (146.90 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3504 mL 11.7520 mL 23.5040 mL
5 mM 0.4701 mL 2.3504 mL 4.7008 mL
10 mM 0.2350 mL 1.1752 mL 2.3504 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.89 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.89 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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BMS-986165
Cat. No.:
HY-117287
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