PROTAC KAT2A/B degrader-1
PROTAC KAT2A/B degrader-1 is an orally active CRBN-baed histone acetyltransferase KAT2A/KAT2B PROTAC degrader. PROTAC KAT2A/B degrader-1 induces degradation of KAT2A and KAT2B proteins. PROTAC KAT2A/B degrader-1 inhibits proliferation of acute myeloid leukemia and small cell lung cancer cells. PROTAC KAT2A/B degrader-1 can be used for the research of acute myeloid leukemia, small cell lung cance.
For research use only. We do not sell to patients.
- CAS No.: 3031606-85-3
- Formula: C31H31ClN6O6
- Molecular Weight:619.07
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Biological Activity
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Cereblon |
PROTAC KAT2A/B degrader-1 (Compound 24) induces potent degradation of KAT2A in MOLM-13 AML cells with a DC50 of 1.53 nM and 90% maximum degradation[1].
PROTAC KAT2A/B degrader-1 induces potent degradation of KAT2A (DC50 = 1.39 nM, Dmax = 95%) and KAT2B (DC50 16.5 nM) in NCI-H1048 SCLC cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 mice[1]
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Dosage:1 mg/kg; 50 mg/kg
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Administration:P.o.; single dose
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Result:Reached a peak free plasma concentration of ~0.01 μM and remained above the H1048 KAT2A DC50 threshold (1.39 nM) through 8 hours, declining thereafter (1 mg/kg dose).
Reached a peak free plasma concentration of ~0.4 μM, remained above the H1048 KAT2A DC90 threshold (22 nM) for at least 24 hours, and demonstrated proportional increases in exposure relative to the 1 mg/kg dose (50 mg/kg dose).
Chemical Information
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CAS No. 3031606-85-3
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Molecular Weight 619.07
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Formula C31H31ClN6O6
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SMILES
CN1C[C@H](NC2=C(Cl)C(N(C)N=C2)=O)C[C@H](C3=CC=C(COC4=CC5=C(C(N(C6C(NC(CC6)=O)=O)C5=O)=O)C=C4)C=C3)C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC KAT2A/B degrader-1 Related Classifications
HY-181695 Related Classifications
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