HAT-SIL-TG-1&AT
HAT-SIL-TG-1&AT is a Janus tyrosine kinase (JAK) inhibitor with antitumor effects. HAT-SIL-TG-1&AT is the hypoxia-activated prodrug, witch inhibits JAK-STAT signaling in tumor tissue. And HAT-SIL-TG-1&AT inhibits HEL cells proliferation and downregulated phosphorylated STAT3/5 under hypoxic conditions.
For research use only. We do not sell to patients.
- CAS No.: 2973282-50-5
- Formula: C60H69N17O11S
- Molecular Weight:1236.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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STAT3 |
STAT5 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEL | IC50 |
>200 μM
Compound: HAT-SIL-TG-1&AT
|
Cytotoxicity against HEL cells assessed as inhibition of cell growth incubated under normoxic condition
Cytotoxicity against HEL cells assessed as inhibition of cell growth incubated under normoxic condition
|
[PMID: 36805946] |
| HEL | IC50 |
3.1 μM
Compound: HAT-SIL-TG-1&AT
|
Cytotoxicity against HEL cells assessed as inhibition of cell growth incubated under hypoxic condition
Cytotoxicity against HEL cells assessed as inhibition of cell growth incubated under hypoxic condition
|
[PMID: 36805946] |
| HUVEC | IC50 |
84.37 μM
Compound: HAT-SIL-TG-1&AT
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Cytotoxicity against HUVEC cells assessed as inhibition of cell growth
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth
|
[PMID: 36805946] |
HAT-SIL-TG-1&AT can be released as TG-1 and AT in the cell lysates under hypoxia condition[1].
HAT-SIL-TG-1&AT (1-5 μM; 24 h) inhibits the phorphoslation of STAT3/5 in HEL cells, and significantly inhibits at 3 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEL cells
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Concentration:3 μM, 5 μM
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Incubation Time:24 h
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Result:Competely inhibited STAT3 phorphoslation at 3 μM and significantly inhibited STAT5 phorphoslation at 5 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HEL tumors xenograft male Balb/c-nude mice[1]
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Dosage:40 mg/kg, 80 mg/kg
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Administration:Intraperitoneal injection; once daily for 14 days
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Result:Resulted regression on tumor growth with TGI values of 88.9% and 91.2%, respectively.
Chemical Information
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CAS No. 2973282-50-5
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Molecular Weight 1236.36
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Formula C60H69N17O11S
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SMILES
CC1=CC(COC(N2C=C(C(C3=NC4=C(N3)C=CC(CN5CCOCC5)=C4)=N2)NC(NC6CC6)=O)=O)=C(C(COC(N7CCN(CC7)C8=CC=C(C=C8)NC9=NC=C(C(NC%10=CC(S(=O)(NC(C)(C)C)=O)=CC=C%10)=N9)C)=O)=C1)OCC%11=CN=C(N%11C)[N+]([O-])=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)