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.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Biological Activity
Description
IC50 & Target
[1]|
Cereblon |
In Vitro
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. Further protocols information, click here.
Parmacokinetics
In Vivo
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.
Protocols
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
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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