DGIdb - TOFACITINIB Drug Record

TOFACITINIB chembl:CHEMBL221959 ApprovedImmunotherapy

Alternate Names:

CP-690
550
CP-690,550 FREE BASE
CP-690550 FREE BASE
CP690550
CP-690-550
CP- 690 550
CP 690550
CP-690,550
CP-690550
TASOCITINIB
CP690,550
TOFACITINIB
XELJANZ®
rxcui:1357536
chemidplus:477600-75-2
drugbank:08895
pubchem.compound:9926791
chembl:CHEMBL221959

Drug Info:

(1 More Sources)

Publications:

Jiang JK et al., 2008, Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550)., J Med Chem
Changelian PS et al., 2003, Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor., Science
Jang WD et al., 2015, Discovery of Tyk2 inhibitors via the virtual site-directed fragment-based drug design., Bioorg Med Chem Lett
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Tan L et al., 2015, Development of Selective Covalent Janus Kinase 3 Inhibitors., J Med Chem
Hou S et al., 2014, Novel carbazole inhibits phospho-STAT3 through induction of protein-tyrosine phosphatase PTPN6., J Med Chem
Koo et al., 2012, Janus kinase 3-activating mutations identified in natural killer/T-cell lymphoma., Cancer Discov
Elliott et al., 2011, FERM domain mutations induce gain of function in JAK3 in adult T-cell leukemia/lymphoma., Blood
Yin et al., 2015, Identification of mutant alleles of JAK3 in pediatric patients with acute lymphoblastic leukemia., Leuk. Lymphoma
Losdyck et al., 2015, Distinct Acute Lymphoblastic Leukemia (ALL)-associated Janus Kinase 3 (JAK3) Mutants Exhibit Different Cytokine-Receptor Requirements and JAK Inhibitor Specificities., J. Biol. Chem.
Degryse et al., 2014, JAK3 mutants transform hematopoietic cells through JAK1 activation, causing T-cell acute lymphoblastic leukemia in a mouse model., Blood

TOFACITINIB STAT5A

Interaction Score: 13.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19053756 14593182

Sources:
DTC
TOFACITINIB STAT5B

Interaction Score: 5.89

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14593182

Sources:
DTC
TOFACITINIB PTPN6

Interaction Score: 4.42

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24978112

Sources:
DTC
TOFACITINIB JAK3

Interaction Score: 3.31

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
14593182 26258521 22705984 21821710 25146434 26446793 25193870 10592235

Sources:
DTC JAX-CKB CIViC TTD
TOFACITINIB TYK2

Interaction Score: 1.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
26231159 10592235

Sources:
DTC
TOFACITINIB JAK2

Interaction Score: 0.43

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

PMIDs:
26258521 10592235

Sources:
DTC
TOFACITINIB YES1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

DTC: TOFACITINIB

Version: 02-September-2020

Alternate Names:

CHEMBL221959 ChEMBL Drug ID

Drug Info:

Publications:

Changelian PS et al., 2003, Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor., Science

Jiang JK et al., 2008, Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550)., J Med Chem

Tan L et al., 2015, Development of Selective Covalent Janus Kinase 3 Inhibitors., J Med Chem

JAX-CKB: Tofacitinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Losdyck et al., 2015, Distinct Acute Lymphoblastic Leukemia (ALL)-associated Janus Kinase 3 (JAK3) Mutants Exhibit Different Cytokine-Receptor Requirements and JAK Inhibitor Specificities., J. Biol. Chem.

Koo et al., 2012, Janus kinase 3-activating mutations identified in natural killer/T-cell lymphoma., Cancer Discov

Elliott et al., 2011, FERM domain mutations induce gain of function in JAK3 in adult T-cell leukemia/lymphoma., Blood

CIViC: TOFACITINIB
- Version: 14-September-2020
Alternate Names:

Drug Info:

Publications:

Degryse et al., 2014, JAK3 mutants transform hematopoietic cells through JAK1 activation, causing T-cell acute lymphoblastic leukemia in a mouse model., Blood
TTD: Tofacitinib
- Version: 2020.06.01
Alternate Names:

D0EG1I TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL221959
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

Indication/Tumor Type	Advanced Solid Tumor
Response Type	sensitive
Approval Status	Preclinical - Cell culture

antagonist (inhibitory)
inhibitor (inhibitory)

TOFACITINIB Drug Record

TOFACITINIB chembl:CHEMBL221959 ApprovedImmunotherapy

Alternate Names:

Drug Info:

Publications:

TOFACITINIB STAT5A

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19053756 14593182

Sources: DTC

TOFACITINIB STAT5B

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 14593182

Sources: DTC

TOFACITINIB PTPN6

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24978112

Sources: DTC

TOFACITINIB JAK3

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type Advanced Solid Tumor Response Type sensitive Approval Status Preclinical - Cell culture

PMIDs: 14593182 26258521 22705984 21821710 25146434 26446793 25193870 10592235

Sources: DTC JAX-CKB CIViC TTD

TOFACITINIB TYK2

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 26231159 10592235

Sources: DTC

TOFACITINIB JAK2

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info:

PMIDs: 26258521 10592235

Sources: DTC

TOFACITINIB YES1

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

DTC: TOFACITINIB

Alternate Names: CHEMBL221959 ChEMBL Drug ID

Drug Info:

JAX-CKB: Tofacitinib

Alternate Names:

Drug Info:

CIViC: TOFACITINIB

Alternate Names:

Drug Info:

Publications: Degryse et al., 2014, JAK3 mutants transform hematopoietic cells through JAK1 activation, causing T-cell acute lymphoblastic leukemia in a mouse model., Blood

TTD: Tofacitinib

Alternate Names: D0EG1I TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL221959

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

n/a

PMIDs:
19053756 14593182

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
14593182

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
24978112

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
14593182 26258521 22705984 21821710 25146434 26446793 25193870 10592235

Sources:
DTC JAX-CKB CIViC TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
26231159 10592235

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

PMIDs:
26258521 10592235

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

CHEMBL221959 ChEMBL Drug ID

Publications:

Degryse et al., 2014, JAK3 mutants transform hematopoietic cells through JAK1 activation, causing T-cell acute lymphoblastic leukemia in a mouse model., Blood

Alternate Names:

D0EG1I TTD Drug ID