2. PROTAC Epigenetics
  3. PROTACs Histone Acetyltransferase
  4. AUR1545

AUR1545 is a selective KAT2A/KAT2B ((GCN5/PCAF)) PROTAC degrader that induces monocyte differentiation and inhibits the growth of acute myeloid leukemia cells. AUR1545 inhibits cell growth, induces epithelial differentiation and suppresses tumor growth in small cell lung cancer models. AUR1545 inhibits cell growth and induces differentiation in neuroendocrine prostate cancer cells and primary patient-derived organoids. AUR1545 is applicable to research related to acute myeloid leukemia, small cell lung cancer and neuroendocrine prostate cancer.
(Pink: GCN5/PCAF ligand (HY-W1122565); Blue: Cereblon ligand (HY-138793); Black: linker).

For research use only. We do not sell to patients.

AUR1545

AUR1545 Chemical Structure

CAS No. : 3031593-79-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
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50 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

AUR1545 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AUR1545 is a selective KAT2A/KAT2B ((GCN5/PCAF)) PROTAC degrader that induces monocyte differentiation and inhibits the growth of acute myeloid leukemia cells. AUR1545 inhibits cell growth, induces epithelial differentiation and suppresses tumor growth in small cell lung cancer models. AUR1545 inhibits cell growth and induces differentiation in neuroendocrine prostate cancer cells and primary patient-derived organoids. AUR1545 is applicable to research related to acute myeloid leukemia, small cell lung cancer and neuroendocrine prostate cancer[1]. (Pink: GCN5/PCAF ligand (HY-W1122565); Blue: Cereblon ligand (HY-138793); Black: linker).

IC50 & Target

GCN5/PCAF

 

Cereblon

 

In Vitro

AUR1545 potently degrades KAT2A/KAT2B and inhibits the growth of NCI-H1048, LASCPC-01 and MOLM-13 cells (1.5 nM, 5 nM, and 1.2 nM, respectively); its DC50 values against KAT2A in the three cell lines are 0.01 nM, 0.67 nM, and 0.11 nM respectively, while its DC50 values against KAT2B are 1.5 nM, 0.16 nM, and 0.075 nM respectively[1].
AUR1545 (0.001-100 nM; 48 h-8 d) induces differentiation in MOLM-13 cells, with an EC50 of 0.3 nM for CD86[1].
AUR1545 (0.01-100 nM; 24 h-7 d) induces epithelial differentiation in LASCPC-01 cells[1].
AUR1545 (0.01-1000 nM; 72 h-21 d) induces microglial differentiation in primary organoids derived from NEPC patients[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AUR1545 Related Antibodies

Cell Viability Assay[1]

Cell Line: ASCPC-01 cells line
Concentration: 0.01 nM, 0.1 nM, 1 nM, 10 nM, 100 nM
Incubation Time: 72 h
Result: Potently degrades KAT2A/KAT2B.
In Vivo

AUR1545 (30 mg/kg; i.p.; once per week) induces 70% tumor growth inhibition and upregulates epithelial differentiation in NCI-H1048 tumor-bearing Nude balb/c mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Small cell lung cancer-brearing nude balb/c mouse model[1]
Dosage: 30 mg/kg
Administration: i.p.; once per week
Result: Achieved 70% tumor growth inhibition (TGI); upregulated epithelial gene set enrichment analysis (GSEA) signatures in treated tumors compared to vehicle controls; reduced KAT2A and KAT2B levels significantly in tumors 168 hours post last dose.
Molecular Weight

828.80

Formula

C41H50BrN9O5
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1NC(C(N2C(C3=C(C=C(C=C3)N4CCN(CC4)CC5CCN(CC5)C(C6=CC=C([C@@H]7CN(C)C[C@H](NC(C=NN8C)=C(Br)C8=O)C7)C=C6)=O)C2)=O)CC1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (120.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2066 mL 6.0328 mL 12.0656 mL
5 mM 0.2413 mL 1.2066 mL 2.4131 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (6.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (6.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2066 mL 6.0328 mL 12.0656 mL 30.1641 mL
5 mM 0.2413 mL 1.2066 mL 2.4131 mL 6.0328 mL
10 mM 0.1207 mL 0.6033 mL 1.2066 mL 3.0164 mL
15 mM 0.0804 mL 0.4022 mL 0.8044 mL 2.0109 mL
20 mM 0.0603 mL 0.3016 mL 0.6033 mL 1.5082 mL
25 mM 0.0483 mL 0.2413 mL 0.4826 mL 1.2066 mL
30 mM 0.0402 mL 0.2011 mL 0.4022 mL 1.0055 mL
40 mM 0.0302 mL 0.1508 mL 0.3016 mL 0.7541 mL
50 mM 0.0241 mL 0.1207 mL 0.2413 mL 0.6033 mL
60 mM 0.0201 mL 0.1005 mL 0.2011 mL 0.5027 mL
80 mM 0.0151 mL 0.0754 mL 0.1508 mL 0.3771 mL
100 mM 0.0121 mL 0.0603 mL 0.1207 mL 0.3016 mL
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AUR1545 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AUR15453031593-79-7AUR 1545AUR-1545PROTACsHistone AcetyltransferaseHATsHATLASCPC-01 cellsprimary patient organoidsacute myeloid leukemiasmall cell lung cancerneuroendocrine prostate cancerNude balb/c miceKAT2ANCI-H1048 cellsKAT2BMOLM-13 cellsInhibitorinhibitorinhibit

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