HM90822
HM90822 is an orally active IAP antagonist. HM90822 induces ubiquitination and proteasome-dependent degradation of XIAP, cIAP1 and cIAP2 in sensitive pancreatic cancer cells. HM90822 induces Apoptotic cell death. HM90822 inhibits tumor growth in Panc-1 pancreatic cancer xenograft and orthotopic mouse models. HM90822 can be used for the research of pancreatic cancer.
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- No. CAS: 1363145-46-3
- Fòrmula: C30H36ClF2N7O4
- Peso molecular:632.11
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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XIAP |
cIAP-1 |
cIAP2 |
HM90822 (72 h) induces dose-dependent cell death in human pancreatic cancer cell lines, with IC50 values of 0.142 μM (BxPC-3), 0.164 μM (Panc03.27), 0.324 μM (Panc-1), 5.3 μM (PL45), and 6.7 μM (Capan-1) after 72 h incubation, while Panc08.13, MiaPaCa-2, Capan-2, and AsPC-1 cells are resistant with IC50 values above 37 μM[1].
HM90822 (0.3-10 μM; 18 h) induces dose-dependent reduction of XIAP and cIAP1 protein expression in sensitive BxPC-3 and Panc-1 human pancreatic cancer cell lines after 18 h incubation, but has no effect on these proteins in resistant MiaPaCa-2 and Capan-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
HM90822 (50-200 mg/kg; p.o.; once daily; for 14 consecutive days) exerts anti-tumor effects in female Balb/c nude mice with Panc-1 orthotopic xenografts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c nude (female)[1]
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Dosage:150 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Reduced tumor size compared to controls.
Did not alter body weight compared to controls.
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Animal Model:Balb/c nude (female)[1]
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Dosage:50 mg/kg; 100 mg/kg; 200 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Significantly reduced intrapancreatic tumor weight at all tested doses compared to controls (P<0.05).
Reduced body weights by approximately 10-20% compared to controls.
Chemical Information
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No. CAS 1363145-46-3
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Peso molecular 632.11
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Fòrmula C30H36ClF2N7O4
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SMILES
N(C=1C2=C(C=C(OC)C(NC(=O)[C@H]3N(C([C@@H](NC([C@@H](NC)C)=O)[C@](C)(C)C)=O)CCC3)=C2)N=CN1)C4=C(F)C(Cl)=C(F)C=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HM90822 Related Classifications
HY-12440 Related Classifications
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