Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C18H16F2N6 |
Molecular Weight | 354.3566 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@H](NC1=C(C=C(F)C(NC2=NNC(C)=C2)=N1)C#N)C3=CC=C(F)C=C3
InChI
InChIKey=SUNXHXDJOIXABJ-NSHDSACASA-N
InChI=1S/C18H16F2N6/c1-10-7-16(26-25-10)23-18-15(20)8-13(9-21)17(24-18)22-11(2)12-3-5-14(19)6-4-12/h3-8,11H,1-2H3,(H3,22,23,24,25,26)/t11-/m0/s1
Molecular Formula | C18H16F2N6 |
Molecular Weight | 354.3566 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/18775810 | https://www.ncbi.nlm.nih.gov/pubmed/21207414Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/21159615
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18775810 | https://www.ncbi.nlm.nih.gov/pubmed/21207414
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/21159615
AZ-960 is a novel inhibitor of janus-associated kinases (JAKs) that exhibits a potent inhibition against janus kinase 2 (JAK2) with the value of inhibition constant of Ki of 0.45 nmol/L. It also exhibits a lesser inhibitory effects against other JAKs family members, including JAK1, JAK3 and TYK2 as well as other kinases, including TrkA, Aurora A and FAK, with 50% inhibition concentration IC50 of around 0.1 umol/L. In recent studies, AZ-960 demonstrates potential anti-cancer activity against adult T-cell leukemia (ATL), an aggressive malignancy of CD4+ T lymphocytes, by effectively inducing growth arrest and apoptosis in human T-cell lumphotropic virus type 1 (HTLV-1) infected T cells. AZ-960 potently inhibited the clonogenic growth and induced apoptosis of freshly isolated AML cells from patients in association with cleavage of caspase 3 and downregulation of anti-apoptotic Bcl-xL proteins.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2971 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18775810 |
0.45 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21159615
AZ-960 (0.03–1 umol/L) suppressed the growth of MT-1 and MT-2 cells with IC50 of 0.8 and 1 umol/L, respectively
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 02:03:41 GMT 2023
by
admin
on
Sat Dec 16 02:03:41 GMT 2023
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Record UNII |
M63IS9PTJF
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Record Status |
Validated (UNII)
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Record Version |
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M63IS9PTJF
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905586-69-8
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DTXSID60238201
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admin on Sat Dec 16 02:03:41 GMT 2023 , Edited by admin on Sat Dec 16 02:03:41 GMT 2023
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