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PWT143, formerly known as ME-401, is an orally bioavailable inhibitor of the delta isoform of phosphatidylinositide 3-kinase (PI3K), with potential antineoplastic activity. The PI3K-delta inhibitor PWT143 selectively inhibits the delta isoform of PI3K after oral administration, preventing the activation of the PI3K/AKT signaling pathway. In tumor cells that overexpress PI3K-delta, this both reduces proliferation and causes cell death. The growth and survival of hematologic cancer cells are significantly influenced by PI3K-delta. In order to maintain PI3K signaling in healthy, non-cancerous cells, PI3K-delta is specifically targeted for inhibition. PI3K, an enzyme that is frequently overexpressed in cancer cells, is essential for the regulation and survival of tumor cells.
| ln Vivo |
ME-401 is an oral, once-daily, selective PI3Kδ inhibitor that is being tested in clinical settings for the treatment of B-cell cancers. It has an ideal pharmacologic profile. To exert its mechanism of action, ME-401 can bind to the target with high affinity, be orally absorbed, spread to the target tissues, enter and accumulate in the target cells, and bind to the target. [2]
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| Animal Protocol |
CD-1 mice, Sprague Dawley (SD) rats, Female BALB/c mice, Beagle dogs, Cynomolgus monkeys
10 mg/kg for mice, 5 mg/kg for rats, 2 mg/kg for dogs and monkeys Oral gavage |
| References |
| Molecular Formula |
C31H40N8O3S
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|---|---|
| Molecular Weight |
604.774
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| Exact Mass |
604.2944
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| Elemental Analysis |
C, 61.57; H, 6.67; N, 18.53; O, 7.94; S, 5.30
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| CAS # |
1595129-71-7
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| Related CAS # |
1595129-71-7;Zandelisib HCl Zandelisib mesylate;
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| Appearance |
Solid powder
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| SMILES |
CC(C)(CC1=CC=CC=C1C2CCN(CC2)C)NC3=NC(=NC(=N3)N4CCOCC4)N5C6=CC=CC=C6N=C5S(=O)(=O)C
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| InChi Key |
PGTXVGREXBMCCY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H40N8O3S/c1-31(2,21-23-9-5-6-10-24(23)22-13-15-37(3)16-14-22)36-27-33-28(38-17-19-42-20-18-38)35-29(34-27)39-26-12-8-7-11-25(26)32-30(39)43(4,40)41/h5-12,22H,13-21H2,1-4H3,(H,33,34,35,36)
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| Chemical Name |
N-[2-methyl-1-[2-(1-methylpiperidin-4-yl)phenyl]propan-2-yl]-4-(2-methylsulfonylbenzimidazol-1-yl)-6-morpholin-4-yl-1,3,5-triazin-2-amine
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| Synonyms |
Zandelisib; PWT-143; PWT143; PWT 143; ME-401; ME 401; ME401
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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: 4.6~20 mg/mL (7.64~33.1mM)
H2O: <0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.44 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 20.8 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: 2.08 mg/mL (3.44 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: ≥ 2.08 mg/mL (3.44 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 | 1.6535 mL | 8.2676 mL | 16.5352 mL | |
| 5 mM | 0.3307 mL | 1.6535 mL | 3.3070 mL | |
| 10 mM | 0.1654 mL | 0.8268 mL | 1.6535 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03985189 | Active Recruiting |
Drug: ME-401 | Relapsed | Kyowa Kirin Co., Ltd. | April 29, 2019 | Phase 1 |
| NCT04533581 | Active Recruiting |
Drug: ME-401 | Indolent B-cell Non-Hodgkin's Lymphoma |
Kyowa Kirin Co., Ltd. | September 17, 2020 | Phase 2 |
| NCT04517435 | Recruiting | Drug: ME-401 Drug: Rituximab |
Diffuse Large B-Cell Lymphoma | Deepa Jagadeesh | April 28, 2021 | Phase 1 Phase 2 |
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