AZD3632
AZD3632 (MLL1-IN-1) is an orally active MLL1 inhibitor with an IC50 of 0.043 μM. AZD3632 induces Menin protein degradation and inhibits the proliferation of leukemia cells. AZD3632 can induce tumor regression in leukemia-bearing mice. AZD3632 is useful for research into MLL1-associated leukemia.
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- CAS. Nr.: 3058433-50-1
- Formel: C34H44FN5O3
- Molecular Weight:589.74
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
In Vitro
AZD3632 (7 days) inhibits the viability of MOLM-13, MV-4-11, and OCI-AML3 cells, with IC50 values of 0.04, 0.035, and 0.047 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AZD3632 (30-200 mg/kg, p.o., once daily for 21/90 days) induces tumor regression in a MOLM-13 subcutaneous xenograft mouse model[1].
AZD3632 (150 mg/kg, p.o., once daily for 21 days) prolongs survival in an MLL-r AML patient-derived xenograft (PDX) mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female CB17 SCID mice with MV-4-11 subcutaneous xenograft[1]
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Dosage:30, 100, 200 mg/kg
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Administration:p.o., twice daily for 14 days
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Result:Reduced tumors by 88%, with a 100% recurrence rate following drug discontinuation at a dose of 30 mg/kg. Reduced tumors by 97%/99%, with no recurrence observed 6 weeks after drug discontinuation at doses of 100/200 mg/kg.
Chemical Information
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CAS. Nr. 3058433-50-1
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Molecular Weight 589.74
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Formel C34H44FN5O3
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SMILES
FC1=CC=[C@]([N@]2C(C=NC=C3)=C3C(C(C4CCN(C([C@@H]5CCC(C)(C)N5)=O)CC4)=O)=C2C)C(C(N(C(C)C)C(C)C)=O)=C1
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Synonyms
MLL1-IN-1
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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
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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