MPC-0767 free base
MPC-0767 free base is an orally active prodrug of Hsp90 inhibitor. MPC-0767 free base undergoes rapid biotransformation to the parent Hsp90 inhibitor MPC-3100 via enzyme-mediated luminal cleavage. MPC-0767 free base is applicable to the research of refractory and recurrent cancers.
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- CAS. Nr.: 1310540-31-8
- Formel: C25H30BrN7O5S
- Molecular Weight:620.52
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
In Vitro
MPC-0767 free base mesylate salt has a half-life of <2 min in mouse plasma, 300 min in monkey plasma, 149 min in human plasma, and 145 min in pH 7.4 phosphate buffer[1].
MPC-0767 free base mesylate salt has a half-life of <2 min in mouse liver microsomes and 2 min in human liver microsomes, with no difference observed between assays run with or without NADPH[1].
MPC-0767 free base mesylate salt is highly stable in simulated gastric fluid but undergoes rapid conversion in pancreatin-containing simulated intestinal fluid with a half-life of 22 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MPC-0767 free base mesylate salt (p.o.; 265 mg/kg) exhibits comparable efficacy in the N-87 xenograft tumor model, inducing a 46% reduction in tumor volume without causing body weight loss[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1310540-31-8
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Molecular Weight 620.52
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Formel C25H30BrN7O5S
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SMILES
C[C@H](N)C(O[C@@H](C)C(N(CC1)CCC1CCN2C3=NC=NC(N)=C3N=C2SC4=C(Br)C=C(OCO5)C5=C4)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Kim SH, et al. Discovery of an L-alanine ester prodrug of the Hsp90 inhibitor, MPC-3100. Bioorganic & medicinal chemistry letters. 2015 Nov 15;25(22):5254-7. [Content Brief]
[2]. Gomez-Monterrey I, et al. Heat shock protein 90 inhibitors as therapeutic agents. Recent patents on anti-cancer drug discovery. 2012 Sep;7(3):313-36. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
MPC-0767 free base Related Classifications
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