| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Additional Infomation |
PCLX-001 is a first-in-class N-myristyltransferase (NMT) inhibitor developed by Pacylex Pharmaceuticals. Existing research indicates that PCLX-001's mechanism of action differs from other known anticancer drugs, demonstrating high activity and positive efficacy in breast, lung, bladder, and pancreatic cancers. Zelenirstat is an orally bioavailable N-myristyltransferase (NMT) inhibitor with potential antitumor activity. After oral administration, Zelenirstat targets and binds to NMT, particularly NMT2. This blocks NMT-mediated signaling and myristylation, thereby inhibiting the proliferation of certain NMT-deficient cancer cells. Zelenirstat also inhibits B-cell receptor (BCR) signaling and reduces the level of Src family tyrosine kinases (SFK). NMTs mediate myristylation, a crucial process through which the fatty acid myristate is added to proteins, enabling them to interact with cell membranes and become part of the cell signaling system. NMT expression is absent in various cancers, such as leukemia cells, which are therefore more sensitive to zelenizal compared to normal cells. The absence of NMT expression may promote tumorigenesis.
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| Molecular Formula |
C24H30CL2N6O2S
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|---|---|
| Molecular Weight |
537.505001544952
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| Exact Mass |
536.152
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| CAS # |
1215011-08-7
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| Related CAS # |
1215011-08-7;DDD86481 Tosylate;
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| PubChem CID |
58561243
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
35
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| Complexity |
781
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WKTSLVQYGBHNRV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H30Cl2N6O2S/c1-15(2)11-21-23(16(3)31(4)29-21)30-35(33,34)24-19(25)12-18(13-20(24)26)17-5-6-28-22(14-17)32-9-7-27-8-10-32/h5-6,12-15,27,30H,7-11H2,1-4H3
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| Chemical Name |
2,6-dichloro-N-[1,5-dimethyl-3-(2-methylpropyl)pyrazol-4-yl]-4-(2-piperazin-1-ylpyridin-4-yl)benzenesulfonamide
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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) |
DMSO : ~10 mg/mL (~18.60 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (1.86 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1 mg/mL (1.86 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 can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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: ≥ 1 mg/mL (1.86 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 | 1.8604 mL | 9.3022 mL | 18.6043 mL | |
| 5 mM | 0.3721 mL | 1.8604 mL | 3.7209 mL | |
| 10 mM | 0.1860 mL | 0.9302 mL | 1.8604 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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