| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
AUR1545 can effectively degrade KAT2A/KAT2B and inhibit the growth of NCI-H1048, LASCPC-01 and MOLM-13 cells (EC50 values of 1.5 nM, 5 nM and 1.2 nM, respectively); its DC50 values for KAT2A in these three cell lines are 0.01 nM, 0.67 nM and 0.11 nM, respectively, and its DC50 values for KAT2B are 1.5 nM, 0.16 nM and 0.075 nM, respectively[1]. AUR1545 (0.001-100 nM; 48 hours-8 days) can induce differentiation of MOLM-13 cells, and its EC50 value for CD86 is 0.3 nM[1]. AUR1545 (0.01-100 nM; 24 hours-7 days) induced epithelial differentiation of LASCPC-01 cells[1]. AUR1545 (0.01-1000 nM; 72 hours-21 days) induced differentiation of primary organoid microglia derived from NEPC patients[1].
|
|---|---|
| ln Vivo |
AUR1545 (30 mg/kg; intraperitoneal injection; once a week) inhibited tumor growth of NCI-H1048 tumors in nude mice balb/c by 70% and upregulated epithelial differentiation [1].
|
| Cell Assay |
Cell viability assay [1]
Cell Types: ASCPC-01 cell line Tested Concentrations: 0.01 nM, 0.1 nM, 1 nM, 10 nM, 100 nM Incubation Duration: 72 hours Experimental Results: Effectively degrades KAT2A/KAT2B. |
| Animal Protocol |
Animal/Disease Models:Small cell lung cancer nude mouse balb/c model [1]
Doses: 30 mg/kg Route of Administration: Intraperitoneal injection; once a week Experimental Results: Tumor growth inhibition rate (TGI) reached 70%; compared with the vector control group, the epithelial gene set enrichment analysis (GSEA) feature in the tumor of the treatment group was upregulated; 168 hours after the last administration, the levels of KAT2A and KAT2B in the tumor were significantly reduced. |
| References |
| Molecular Formula |
C41H50BRN9O5
|
|---|---|
| Molecular Weight |
828.80
|
| CAS # |
3031593-79-7
|
| Appearance |
Off-white to light yellow solid
|
| 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
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~120.66 mM; with sonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (6.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (50.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in double-distilled water and dilute to 100 mL to obtain clear physiological saline. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (6.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (50.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD saline (4°C, store for one week): Dissolve 2 g of SBE-β-CD powder in 10 mL of saline until completely dissolved and clear. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (6.03 mM)(saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1207 mL | 0.6033 mL | 1.2066 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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