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PROTAC KAT2A/B degrader-1
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Catalog No. T218810 Copy Product Info
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PROTAC KAT2A/B degrader-1 is an orally active histone acetyltransferase KAT2A/KAT2B PROTAC degrader. It facilitates the degradation of KAT2A and KAT2B proteins and inhibits the proliferation of acute myeloid leukemia and small cell lung cancer cells. PROTAC KAT2A/B degrader-1 is applicable in research related to acute myeloid leukemia and small cell lung cancer.
PROTAC KAT2A/B degrader-1
Cas No. 3031606-85-3
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | PROTAC KAT2A/B degrader-1 is an orally active histone acetyltransferase KAT2A/KAT2B PROTAC degrader. It facilitates the degradation of KAT2A and KAT2B proteins and inhibits the proliferation of acute myeloid leukemia and small cell lung cancer cells. PROTAC KAT2A/B degrader-1 is applicable in research related to acute myeloid leukemia and small cell lung cancer. |
| In vitro | PROTAC KAT2A/B degrader-1 (Compound 24) effectively degrades KAT2A in MOLM-13 acute myeloid leukemia (AML) cells, with a DC50 of 1.53 nM and a maximum degradation rate of 90%. In NCI-H1048 SCLC cells, PROTAC KAT2A/B degrader-1 strongly degrades KAT2A (DC50 = 1.39 nM, Dmax = 95%) and KAT2B (DC50 = 16.5 nM). |
| In vivo | Compound PROTAC KAT2A/B degrader-1 (Compound 24) administered orally at doses ranging from 1-50 mg/kg in a single dose achieves and maintains free plasma concentrations above the H1048 KAT2A DC 90 threshold (22 nM) for at least 24 hours at a 50 mg/kg dose in CD-1 mice. |
| Molecular Weight | 619.07 |
| Formula | C31H31ClN6O6 |
| Cas No. | 3031606-85-3 |
| Smiles | O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=C(OCC4=CC=C(C=C4)[C@H]5C[C@@H](NC6=C(Cl)C(=O)N(C)N=C6)CN(C)C5)C2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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Related Tags: PROTAC KAT2A/B degrader-1 in vivo | PROTAC KAT2A/B degrader-1 in vitro | PROTAC KAT2A/B degrader-1 formula | PROTAC KAT2A/B degrader-1 molecular weight
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