GL392
GL392 is a senolytic agent that selectively delivers the potent senolytic compound Dasatinib (HY-10181) to senescent cells. GL392 targets lipofuscin in senescent cells via the LBD domain and is linked to Dasatinib through an ester bond. Upon internalization in senescent cells, Dasatinib is released, inducing apoptosis of the senescent cells. GL392 in micelle encapsulation (mGL392) enables selective delivery to senescent cells, achieving selective senescent cell elimination in vitro and in vivo. GL392 can be used for the research of melanoma.
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- 화학식: C55H52ClN13O5S
- 분자량:1042.60
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
mGL392 (20-160 nM, 4 days) does not affect non-senescent B16 melanoma growth[1].
mGL392 (10 nM) selectively accumulates within senescent cells in HBEC CDC6 Tet-ON and Li-Fraumeni-p21WAF1/Cip1 Tet-ON cells[1].
mGL392 (500 nM, 4 days) induces targeted senolysis in 3D patient-derived lung organoids[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:B16 cells
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Concentration:20, 80, 160 nM
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Incubation Time:4 days
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Result:Showed no affect on non-senescent B16 melanoma growth.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (8-10 weeks old) subcutaneously injected with B16 melanoma cells, followed by Palbociclib-induced senescence[1]
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Dosage:0.015 mg per mouse
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Administration:i.p.; daily; 9 days
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Result:Reduced tumor volume significantly.
Induced tumor cell apoptosis.
Did not affect non-senescent B16 melanoma cell viability in vivo when senescence was absent.
Left serum markers of liver, kidney, and muscle function (including ALP, AST/ALT ratio, and CPK) within normal ranges, with no histopathological damage to vital organs observed.
Chemical Information
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분자량 1042.60
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화학식 C55H52ClN13O5S
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SMILES
CC1(COC(CCC(OCCN2CCN(C3=CC(NC4=NC=C(C(NC5=C(C)C=CC=C5Cl)=O)S4)=NC(C)=N3)CC2)=O)=O)NC6=CC=CC(C6=C(N1)C=C7)=C7/N=N/C(C=C8)=C9C(C=CC=C9)=C8/N=N/C%10=CC=CC=C%10
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)