1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
    Metabolic Enzyme/Protease
  2. JAK
    Cytochrome P450
  3. BMS-986202

BMS-986202 

Cat. No.: HY-131968
Handling Instructions

BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is remarkably selective over other kinases including Jak family members. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 of 14 μM. BMS-986202 can be used for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus research.

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

BMS-986202 Chemical Structure

BMS-986202 Chemical Structure

CAS No. : 1771691-34-9

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Description

BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is remarkably selective over other kinases including Jak family members. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 of 14 μM. BMS-986202 can be used for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus research[1].

IC50 & Target[1]

Tyk2 JH2

0.19 nM (IC50)

Tyk2 JH2

0.02 nM (Ki)

CYP2C19

14 μM (IC50)

In Vitro

BMS-986202 inhibits IFNα and IL-23 in Kit225 T cells with IC50 values of 10 nM and 12 nM, respectively[1].
BMS-986202 is potent in the IFNα stimulated STAT5 phosphorylation human whole blood (hWB) assay and mouse whole blood (mWB) with IC50 values of 58 nM and 481 nM, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

BMS-986202 (Compound 7; 3-30 mg/kg; p.o.; daily; for 9 days) treatment inhibits IL-23-driven acanthosis in mice[1].
BMS-986202 (Compound 7; 0.4-10 mg/kg; p.o.) treatment inhibits IL-12/IL-18-induced IFNγ production in mice. BMS-986202 dose-dependently inhibits IFNγ production by 46% and 80% at doses of 2 mg/kg and 10 mg/kg, respectively[1].
BMS-986202 (Compound 7; 7-10 mg/kg; p.o.) is stable in liver microsomes, with half lives of greater than 120 min in mouse, rat, monkey, and humans and 89 min in dog. The serum protein binding for BMS-986202 in these species ranges from 89.3% to 96.0%, leaving a good range of free fraction of drug available. BMS-986202 shows the oral bioavailability up to 62-100%[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 female mice (9-11 weeks) injected with IL-23[1]
Dosage: 3 mg/kg, 10 mg/kg, and 30 mg/kg
Administration: Oral administration; daily; for 9 days
Result: Inhibited ear swelling in a dose-responsive manner in IL-23-induced acanthosis in mice.
Molecular Weight

439.46

Formula

C₂₂H₁₈D₃FN₆O₃

CAS No.

1771691-34-9

SMILES

O=C(NC1=NC=C(C(NC2=CC=CC(C3=NC=C(C=N3)F)=C2OC)=C1)C(NC([2H])([2H])[2H])=O)C4CC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

BMS-986202BMS986202BMS 986202JAKCytochrome P450Janus kinaseCYPsTyk2JH2IL-23IL-12IFNγacanthosiscolitisspontaneous lupusInhibitorinhibitorinhibit

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Product Name:
BMS-986202
Cat. No.:
HY-131968
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