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Art. -Nr.: HY-149257

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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.

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CAS. Nr.: 2973282-50-5
Formel: C₆₀H₆₉N₁₇O₁₁S
Molecular Weight:1236.36

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

HAT-SIL-TG-1&AT Chemical Structure

CAS. Nr.: 2973282-50-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

STAT3

STAT5

Alle JAK Isoform-spezifische Produkte anzeigen :

Alle STAT Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	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	Cytotoxicity against HUVEC cells assessed as inhibition of cell growth Cytotoxicity against HUVEC cells assessed as inhibition of cell growth	[PMID: 36805946]

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

HEL cells
Concentration:

3 μM, 5 μM
Incubation Time:

24 h
Result:

Competely inhibited STAT3 phorphoslation at 3 μM and significantly inhibited STAT5 phorphoslation at 5 μM.

In Vivo

HAT-SIL-TG-1&AT (80 mg/kg; ip; once daily for 14 days) exhibits significant tumor growth inhibition in HEL tumors xenograft male Balb/c-nude mice. HAT-SIL-TG-1&AT also induces cell apoptosis in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

HEL tumors xenograft male Balb/c-nude mice^[1]
Dosage:

40 mg/kg, 80 mg/kg
Administration:

Intraperitoneal injection; once daily for 14 days
Result:

Resulted regression on tumor growth with TGI values of 88.9% and 91.2%, respectively.

Chemical Information

CAS. Nr. 2973282-50-5
Molecular Weight 1236.36
Formel C₆₀H₆₉N₁₇O₁₁S
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Chen X, et al. A JAK tyrosine kinase and pseudokinase Co-inhibition strategy combines enhanced potency and on-demand activation. Eur J Med Chem. 2023 Mar 15;250:115198. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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HAT-SIL-TG-1&AT

Alle JAK Isoform-spezifische Produkte anzeigen

Alle STAT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

HAT-SIL-TG-1&AT Related Classifications

HY-149257 Related Classifications