| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
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| Targets |
Bcl-xL
|
|---|---|
| ln Vitro |
Using the mitochondrial route, PZ703b hydrochloride (0–1 μM, 24 hours) works in concert with Mivebresib to prevent bladder cancer cell growth and trigger apoptosis in bladder cancer cells [1]. With IC50 values of 15.9 and 11.3 nM, respectively, PZ703b hydrochloride (0-1 μM, 48 h) suppresses the cell activity of MOLT-4 and RS4;11[2]. Through the caspase-3-mediated route, PZ703b hydrochloride (10 nM, 48 h) causes BCL-XL degradation and death in MOLT-4 cells [2].
|
| Cell Assay |
Apoptosis Analysis[1]
Cell Types: MOLT-4 cell line Tested Concentrations: 10 μM Incubation Duration: 48 hrs (hours) Experimental Results: Induced cell apoptosis of MOLT-4 cells. |
| References |
[1]. Yi Xu, et al. Mivebresib synergized with PZ703b, a novel Bcl-xl PROTAC degrader, induces apoptosis in bladder cancer cells via the mitochondrial pathway. Biochem Biophys Res Commun. 2022 Oct 1;623:120-126.
[2]. Pratik Pal, et al. Discovery of a Novel BCL-XL PROTAC Degrader with Enhanced BCL-2 Inhibition. J Med Chem. 2021 Oct 14;64(19):14230-14246. |
| Molecular Formula |
C80H103CL2F3N10O11S4
|
|---|---|
| Related CAS # |
PZ703b;2471970-56-4;PZ703b TFA
|
| Appearance |
Typically exists as solid at room temperature
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 :~180 mg/mL (~109.96 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4.5 mg/mL (2.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 can add 100 μL of 45.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 4.5 mg/mL (2.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 can add 100 μL of 45.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
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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