Product Name :
BMS-986202
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.
CAS:
1771691-34-9
Molecular Weight:
439.46
Formula:
C22H21FN6O3
Chemical Name:
6-cyclopropaneamido-4-{[3-(5-fluoropyrimidin-2-yl)-2-methoxyphenyl]amino}-N-(²H₃)methylpyridine-3-carboxamide
Smiles :
[2H]C([2H])([2H])NC(=O)C1=CN=C(C=C1NC1=CC=CC(C2N=CC(F)=CN=2)=C1OC)NC(=O)C1CC1
InChiKey:
BBRMAVGRWHNAIG-FIBGUPNXSA-N
InChi :
InChI=1S/C22H21FN6O3/c1-24-22(31)15-11-25-18(29-21(30)12-6-7-12)8-17(15)28-16-5-3-4-14(19(16)32-2)20-26-9-13(23)10-27-20/h3-5,8-12H,6-7H2,1-2H3,(H,24,31)(H2,25,28,29,30)/i1D3
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.{{Rebamipide} medchemexpress|{Rebamipide} Immunology/Inflammation|{Rebamipide} Protocol|{Rebamipide} In Vitro|{Rebamipide} supplier|{Rebamipide} Epigenetics}
Additional information:
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.|Product information|CAS Number: 1771691-34-9|Molecular Weight: 439.46|Formula: C22H21FN6O3|Chemical Name: 6-cyclopropaneamido-4-{[3-(5-fluoropyrimidin-2-yl)-2-methoxyphenyl]amino}-N-(²H₃)methylpyridine-3-carboxamide|Smiles: [2H]C([2H])([2H])NC(=O)C1=CN=C(C=C1NC1=CC=CC(C2N=CC(F)=CN=2)=C1OC)NC(=O)C1CC1|InChiKey: BBRMAVGRWHNAIG-FIBGUPNXSA-N|InChi: InChI=1S/C22H21FN6O3/c1-24-22(31)15-11-25-18(29-21(30)12-6-7-12)8-17(15)28-16-5-3-4-14(19(16)32-2)20-26-9-13(23)10-27-20/h3-5,8-12H,6-7H2,1-2H3,(H,24,31)(H2,25,28,29,30)/i1D3|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 250 mg/mL (568.{{Desloratadine} MedChemExpress|{Desloratadine} GPCR/G Protein|{Desloratadine} Technical Information|{Desloratadine} In stock|{Desloratadine} manufacturer|{Desloratadine} Epigenetics} 88 mM; Need ultrasonic).PMID:26446225 |Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|BMS-986202 inhibits IFNα and IL-23 in Kit225 T cells with IC50 values of 10 nM and 12 nM, respectively. 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.|In Vivo:|BMS-986202 (Compound 7; 3-30 mg/kg; p.o.; daily; for 9 days) treatment inhibits IL-23-driven acanthosis in mice. 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. 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%.|Products are for research use only. Not for human use.|