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ChemicalBook--->CAS DataBase List--->882290-02-0

882290-02-0

882290-02-0 Structure

882290-02-0 Structure
IdentificationBack Directory
[Name]

SC-99
[CAS]

882290-02-0
[Synonyms]

SC-99
N'-(3-Chloro-4-fluorophenyl)-2-(4-chlorophenyl)-2-oxoacetohydrazonoyl cyanide
N'-(3-Chloro-4-fluorophenyl)-2-(4-chlorophenyl)-2-oxoacetohydrazonoyl cyanide
2-(2-(3-Chloro-4-fluorophenyl)hydrazono)-3-(4-chlorophenyl)-3-oxo-propanenitrile
Benzenepropanenitrile, 4-chloro-α-[2-(3-chloro-4-fluorophenyl)hydrazinylidene]-β-oxo-
orally,ERK,c-Src,SC 99,ATP-binding,phosphorylation,platelet,AKT,Janus kinase,activation,anti-myeloma,mTOR,anti-thrombotic,Inhibitor,myeloma,pocket,SC99,multiple,aggregation,STAT,OPM2,JAK,SC-99,Apoptosis,inhibit
[Molecular Formula]

C15H8Cl2FN3O
[MOL File]

882290-02-0.mol
[Molecular Weight]

336.15
Chemical PropertiesBack Directory
[Boiling point ]

459.4±55.0 °C(Predicted)
[density ]

1.38±0.1 g/cm3(Predicted)
[form ]

Solid
[pka]

4.83±0.10(Predicted)
[color ]

Light yellow to yellow
Hazard InformationBack Directory
[Uses]

SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 docks into the ATP-binding pocket of JAK2. SC99 inhibits phosphorylation of JAK2 and STAT3 with no effects on the other kinases associated with STAT3 signaling. SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities[1][2][3].
[in vivo]

SC99 (30 mg/kg; orally; daily; for continuous 14 or 28 days) delays myeloma tumor growth in xenograft mice models[1].
SC99 (5, 10,?15 mM, 15?μL; ICV) produces an effective inhibitory effect on the phosphorylation of JAK2 and STAT3 in middle cerebral artery occlusion and reperfusion (MCAO/R) model (adult male SD rats; 250-300?g). SC99 ameliorates neuronal apoptosis and degeneration, neurobehavioral deficits, inflammatory response and brain edema[3].

Animal Model:Nude mice with Human MM cells OPM2 or JJN3[1]
Dosage:30 mg/kg
Administration:Orally; daily; for continuous 14 or 28 days
Result:Delayed myeloma tumor growth in xenograft mice models and suppressed tumor growth more than 40% in 14 days in the OPM2 model.
[IC 50]

STAT3; JAK2
[References]

[1] Zubin Zhang, et al. A novel small molecule agent displays potent anti-myeloma activity by inhibiting the JAK2-STAT3 signaling pathway. Oncotarget. 2016 Feb 23;7(8):9296-308. DOI:10.18632/oncotarget.6974
[2] Zhuan Xu, et at. A novel STAT3 inhibitor negatively modulates platelet activation and aggregation. Acta Pharmacol Sin. 2017 May;38(5):651-659. DOI:10.1038/aps.2016.155
[3] Yiping Ding, et al. Effects of SC99 on cerebral ischemia-perfusion injury in rats: Selective modulation of microglia polarization to M2 phenotype via inhibiting JAK2-STAT3 pathway. Neurosci Res. 2019 May;142:58-68. DOI:10.1016/j.neures.2018.05.002
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