| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
APO-50815 (compound 14) effectively inhibits recombinant human WEE1 kinase with an IC50 value of 9 nM. It is 10 times more selective for WEE1 than PLK1 and has no activity against CHK1 at concentrations up to 10 μM [1]. APO-50815 (100 pM-100 μM; 5 days) effectively reduces the activity of TP53-mutant peritoneal metastatic CRC organoid cell lines PM003 (IC50 = 37 nM) and PM025 (IC50 = 74 nM), and its efficacy is superior to clinical and preclinical WEE1 inhibitors [1]. APO-50815 (100 pM-100 μM; 5 days) effectively reduced the viability of the TP53 mutant liver metastatic CRC organoid cell line QEH039LM (IC50 = 50 nM), and showed enhanced activity against the KRASG12X mutant, WEE1 inhibitor-resistant cell line QEH042LM (IC50 = 633 nM), which was superior to clinical WEE1 inhibitors [1]. APO-50815 (100 pM-100 μM; 5 days) effectively and selectively reduced the viability of primary CRC organoids with different mutation profiles, and had extremely high therapeutic indices of 238 (RAH051), 146 (RAH035) and 129 (RAH057), respectively [1]. APO-50815 (300 nM; 48 hours) significantly reduced the active cell cycle of TP53-WT and BRAFV600E primary CRC organoid cell lines RAH051T, exacerbated DNA damage and S-phase cell accumulation, and enhanced apoptosis [1]. APO-50815 (90 nM; 2 hours) significantly reduced the level of pTyr15-CDK1 in MDA-MB-231HM cells, confirming its binding to the intracellular WEE1 target and its inhibitory effect [1]. APO-50815 (1 μM; 37 °C for up to 60 minutes) showed poor metabolic stability, short half-life, and high intrinsic clearance rate in human and mouse liver microsomes, indicating that it was rapidly metabolized [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: CRC organoid lines PM003 and PM025; TP53 mutant liver metastatic CRC organoid line QEH039LM; primary CRC organoids Tested Concentrations: 0.1 nM; 1 nM; 10 nM; 100 nM; 1 μM; 10 μM; 100 μM Incubation Duration: 5 days Experimental Results: Effectively reduced the viability of TP53 mutant peritoneal metastatic CRC organoid lines PM003 (IC50 = 37 nM) and PM025 (IC50 = 74 nM). This compound significantly reduced the activity of the TP53-mutant liver metastatic CRC organoid cell line QEH039LM (IC50 = 50 nM) and exhibited enhanced activity against the KRASG12X-mutant, WEE1 inhibitor-resistant cell line QEH042LM (IC50 = 633 nM). This compound effectively and selectively reduced the activity of primary CRC organoids with different mutation profiles and possessed extremely high therapeutic indices of 238 (RAH051), 146 (RAH035), and 129 (RAH057), respectively. Cell cycle analysis [1] Cell Types: TP53-WT, BRAFV600E primary CRC organoid line RAH051T Tested Concentrations: 300 nM Incubation Duration: 48 hours Experimental Results: Significantly reduced the cell cycle of viable cells, exacerbated DNA damage and S phase accumulation, and enhanced apoptosis. Western Blot Analysis [1] Cell Types: TP53-mutant MDA-MB-231HM triple-negative breast cancer cells Tested Concentrations: 90 nM Incubation Duration: 2 hours Experimental Results: pTyr15-CDK1 levels were significantly reduced, confirming the functional inhibition of WEE1 activity and successful penetration of the cell membrane to bind to the target. |
| References |
| Molecular Formula |
C28H29N7O2S
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|---|---|
| Molecular Weight |
527.64
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| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
C=CCN1C(C2=CN=C(N=C2N1C3=CC=CC(C4(CSC4)O)=N3)NC5=CC6=C(C7(CN(C6)C)CC7)C=C5)=O
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8952 mL | 9.4762 mL | 18.9523 mL | |
| 5 mM | 0.3790 mL | 1.8952 mL | 3.7905 mL | |
| 10 mM | 0.1895 mL | 0.9476 mL | 1.8952 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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