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Baricitinib - ≥99%, high purity , Tyrosine-protein kinase JAK2 inhibitor, CAS No.1187594-09-7, Tyrosine-protein kinase JAK2 inhibitor

  • Moligand™
  • ≥99%
Item Number
B127687
Grouped product items
SKUSizeAvailabilityPrice Qty
B127687-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$33.90
B127687-10mg
10mg
In stock
$51.90
B127687-50mg
50mg
In stock
$198.90
B127687-250mg
250mg
In stock
$893.90
B127687-1g
1g
In stock
$3,216.90

Highly potent JAK1 and JAK2 inhibitor; also inhibits JAK3 and Tyk2

Basic Description

SynonymsBaricitinib|1187594-09-7|olumiant|INCB028050|LY3009104|INCB 028050|2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(ethylsulfonyl)azetidin-3-yl)acetonitrile|INCB-028050|UNII-ISP4442I3Y|LY-3009104|ISP4442I3Y|Baricitinib [USAN:INN]|1-(Ethylsulf
Specifications & PurityMoligand™, ≥99%
Biochemical and Physiological MechanismsHighly potent JAK1 and JAK2 inhibitor (IC50values are 5.9 and 5.7 nM, respectively). Also inhibits Tyk2 (IC50= 53 nM). Displays >100-fold selectivity for JAK1/2 over JAK3 (IC50= 53 nM for JAK3). Binds AAK1, BIKE, GAK and MPSK1in vitro(Kdvalues are 17.2, 3
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionTyrosine-protein kinase JAK2 inhibitor
Note5mg、10mg卖完停产,不再备货
Product Description

Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2.
A selective inhibitor of JAK1 and JAK2.

Product Properties

ALogP-0.5

Associated Targets

CTH Tchem Cystathionine gamma-lyase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK1 Tchem Cyclin-dependent kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

EPHB6 Tchem Ephrin type-B receptor 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GABRA1 Tclin Gamma-aminobutyric acid receptor subunit alpha-1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

EGFR Tclin Epidermal growth factor receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DNAJA1 Tchem DnaJ homolog subfamily A member 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK9 Tchem Cyclin-dependent kinase 9 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK5 Tchem Cyclin-dependent-like kinase 5 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

YES1 Tclin Tyrosine-protein kinase Yes 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TYK2 Tclin Non-receptor tyrosine-protein kinase TYK2 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FGFR1 Tclin Fibroblast growth factor receptor 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MET Tclin Hepatocyte growth factor receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

IGF1R Tclin Insulin-like growth factor 1 receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PRKACG Tchem cAMP-dependent protein kinase catalytic subunit gamma 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SLC6A3 Tclin Sodium-dependent dopamine transporter 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SLC6A4 Tclin Sodium-dependent serotonin transporter 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PLK4 Tchem Serine/threonine-protein kinase PLK4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIM1 Tchem Serine/threonine-protein kinase pim-1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PTGS1 Tclin Prostaglandin G/H synthase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BTK Tclin Tyrosine-protein kinase BTK 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ATR Tchem Serine/threonine-protein kinase ATR 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKB Tchem Aurora kinase B 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DRD3 Tclin D(3) dopamine receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AAK1 Tchem AP2-associated protein kinase 1 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TNK2 Tclin Activated CDC42 kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ACHE Tclin Acetylcholinesterase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ACVRL1 Tchem Serine/threonine-protein kinase receptor R3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AKT3 Tchem RAC-gamma serine/threonine-protein kinase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRA1A Tclin Alpha-1A adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AKT2 Tchem RAC-beta serine/threonine-protein kinase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AR Tclin Androgen receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AKT1 Tchem RAC-alpha serine/threonine-protein kinase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAOA Tclin Amine oxidase [flavin-containing] A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADORA1 Tclin Adenosine receptor A1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR1A Tclin 5-hydroxytryptamine receptor 1A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR2B Tclin 5-hydroxytryptamine receptor 2B 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

F2 Tclin Prothrombin 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CLK3 Tchem Dual specificity protein kinase CLK3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CLK1 Tchem Dual specificity protein kinase CLK1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

OPRM1 Tclin Mu-type opioid receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

Pubchem Sid488200979
Pubchem Sid Urlhttps://pubchem.ncbi.nlm.nih.gov/substance/488200979
IUPAC Name 2-[1-ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile
INCHI InChI=1S/C16H17N7O2S/c1-2-26(24,25)22-9-16(10-22,4-5-17)23-8-12(7-21-23)14-13-3-6-18-15(13)20-11-19-14/h3,6-8,11H,2,4,9-10H2,1H3,(H,18,19,20)
InChi Key XUZMWHLSFXCVMG-UHFFFAOYSA-N
Canonical SMILES CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3
Isomeric SMILES CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3
PubChem CID 44205240
Molecular Weight 371.42

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

10 results found

Lot NumberCertificate TypeDateItem
B1512012Certificate of AnalysisApr 02, 2024 B127687
G2304206Certificate of AnalysisMay 31, 2023 B127687
G2304222Certificate of AnalysisMay 31, 2023 B127687
G2304223Certificate of AnalysisMay 31, 2023 B127687
G2304224Certificate of AnalysisMay 31, 2023 B127687
G2304242Certificate of AnalysisMay 31, 2023 B127687
G2304250Certificate of AnalysisMay 31, 2023 B127687
G2304283Certificate of AnalysisMay 31, 2023 B127687
G2304287Certificate of AnalysisMay 31, 2023 B127687
G2304303Certificate of AnalysisMay 31, 2023 B127687

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 37.14, Max Conc. mM: 100

Safety and Hazards(GHS)

Pictogram(s) GHS08,   GHS09,   GHS07
Signal Danger
Hazard Statements

H373:Causes damage to organs through prolonged or repeated exposure

H411:Toxic to aquatic life with long lasting effects

H302:Harmful if swallowed

H360:May damage fertility or the unborn child

Precautionary Statements

P273:Avoid release to the environment.

P280:Wear protective gloves/protective clothing/eye protection/face protection.

P405:Store locked up.

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P260:Do not breathe dust/fume/gas/mist/vapors/spray.

P270:Do not eat, drink or smoke when using this product.

P391:Collect spillage.

P330:Rinse mouth.

P203:Obtain, read and follow all safety instructions before use.

P301+P317:IF SWALLOWED: Get medical help.

P318:if exposed or concerned, get medical advice.

P319:Get medical help if you feel unwell.

Related Documents

References

1. Fridman JS, Scherle PA, Collins R, Burn TC, Li Y, Li J, Covington MB, Thomas B, Collier P, Favata MF et al..  (2010)  Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050..  J Immunol,  184  (9): (5298-307).  [PMID:20363976]
2. Genovese MC, Kremer J, Zamani O, Ludivico C, Krogulec M, Xie L, Beattie SD, Koch AE, Cardillo TE, Rooney TP et al..  (2016)  Baricitinib in Patients with Refractory Rheumatoid Arthritis..  N Engl J Med,  374  (13): (1243-52).  [PMID:27028914]
3. Kennedy Crispin M, Ko JM, Craiglow BG, Li S, Shankar G, Urban JR, Chen JC, Cerise JE, Jabbari A, Winge MC et al..  (2016)  Safety and efficacy of the JAK inhibitor tofacitinib citrate in patients with alopecia areata..  JCI Insight,  (15): (e89776).  [PMID:27699252]
4. Mackay-Wiggan J, Jabbari A, Nguyen N, Cerise JE, Clark C, Ulerio G, Furniss M, Vaughan R, Christiano AM, Clynes R.  (2016)  Oral ruxolitinib induces hair regrowth in patients with moderate-to-severe alopecia areata..  JCI Insight,  (15): (e89790).  [PMID:27699253]
5. Xing L, Dai Z, Jabbari A, Cerise JE, Higgins CA, Gong W, de Jong A, Harel S, DeStefano GM, Rothman L et al..  (2014)  Alopecia areata is driven by cytotoxic T lymphocytes and is reversed by JAK inhibition..  Nat Med,  20  (9): (1043-9).  [PMID:25129481]
6. Jabbari A, Dai Z, Xing L, Cerise JE, Ramot Y, Berkun Y, Sanchez GA, Goldbach-Mansky R, Christiano AM, Clynes R et al..  (2015)  Reversal of Alopecia Areata Following Treatment With the JAK1/2 Inhibitor Baricitinib..  EBioMedicine,  (4): (351-5).  [PMID:26137574]
7. Richardson P, Griffin I, Tucker C, Smith D, Oechsle O, Phelan A, Stebbing J.  (2020)  Baricitinib as potential treatment for 2019-nCoV acute respiratory disease..  Lancet,  395  (10223): (e30-e31).  [PMID:32032529]
8. Stebbing J, Phelan A, Griffin I, Tucker C, Oechsle O, Smith D, Richardson P.  (2020)  COVID-19: combining antiviral and anti-inflammatory treatments..  Lancet Infect Dis,  20  (4): (400-402).  [PMID:32113509]

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