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| 5mg |
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| 25mg |
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Purity: ≥98%
Linperlisib (YY20394; PI3Kδ-IN-2)is a novel, potent, orally bioavailable, and highly selective PI3Kδ inhibitor that was being investigated in a phase I trial for patients with relapse or refractory B-cell malignancies. In vitro and in vivo growth inhibition of PI3K-expressing human tumor cells was achieved with the development of YY-20394. In immune-competent mice with 4T1 and CT26 tumors, YY-20394 also significantly reduced lung metastasis of 4T1 tumors with dose-dependent inhibition. T cells acted as a major mediator for YY-20394's anti-tumor effectiveness. More significantly, YY-20394 achieved long-term immune memory that is specific for CT26 tumors but not for unrelated A20 tumors, and it synergistically improved the anti-tumor efficacy of anti-PD-L1 antibody in the CT26 model. In vitro mechanistic studies revealed that YY-20394 significantly reduced T cell differentiation into Treg in both mouse splenocytes and primary CD4+ T cells from humans. It was also particularly effective at reducing their in vitro IL-10 secretion. Analysis of tumors treated with YY-20394 revealed that the drug reduced IL-10 secretion as well as the proportion of Treg in the leukocytes infiltrating the tumor. Additionally, it had some effects on the tumors' myeloid populations. These findings imply that the novel PI3Kδ inhibitor YY-20394 is a promising and secure immune modulator with significant promise as a cancer immunotherapeutic.
| Targets |
PI3Kδ (IC50 = 6.4 nM)
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|---|---|
| ln Vitro |
Linperlisib (YY-20394) is under the study for follicular lymphoma that is recurrent and/or resistant.
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| References | |
| Additional Infomation |
Linperlisib is an orally available selective inhibitor of the delta form of phosphatidylinositol 3-kinase (PI3-kinase subunit delta; PI3K-delta; PI3Kdelta), with potential antineoplastic activity. Upon oral administration linperlisib selectively binds to and inhibits PI3K-delta and prevents the activation of the PI3K/AKT signaling pathway. This decreases proliferation of and induces cell death in PI3K-delta over-expressing tumor cells. PI3K-delta also plays a key role in the B-cell receptor (BCR) signaling pathway and the proliferation of certain hematologic cancer cells. The targeted inhibition of PI3K-delta is designed to preserve PI3K signaling in normal, non-neoplastic cells, thereby minimizing serious side effects.
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| Molecular Formula |
C28H37FN6O5S
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|---|---|
| Molecular Weight |
588.6940
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| Exact Mass |
588.253
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| Elemental Analysis |
C, 57.13; H, 6.34; F, 3.23; N, 14.28; O, 13.59; S, 5.45
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| CAS # |
1702816-75-8
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| Related CAS # |
1702816-75-8;Unknown (HCl);
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| PubChem CID |
91754520
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
41
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| Complexity |
958
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NVWKNQGHVMMAJW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H37FN6O5S/c1-28(2,36)20-5-7-34(8-6-20)17-19-13-21(29)15-22-24(31-27(32-25(19)22)35-9-11-40-12-10-35)18-14-23(33-41(4,37)38)26(39-3)30-16-18/h13-16,20,33,36H,5-12,17H2,1-4H3
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| Chemical Name |
N-[5-[6-fluoro-8-[[4-(2-hydroxypropan-2-yl)piperidin-1-yl]methyl]-2-morpholin-4-ylquinazolin-4-yl]-2-methoxypyridin-3-yl]methanesulfonamide
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| Synonyms |
PI3Kδ-IN-2; Linperlisib; YY20394; YY 20394; YY-20394
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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: ~100 mg/mL (~169.9 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.25 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 25.0 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: ≥ 2.5 mg/mL (4.25 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 25.0 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: ≥ 2.5 mg/mL (4.25 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 | 1.6987 mL | 8.4934 mL | 16.9869 mL | |
| 5 mM | 0.3397 mL | 1.6987 mL | 3.3974 mL | |
| 10 mM | 0.1699 mL | 0.8493 mL | 1.6987 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 | Status | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05429398 | Not yet recruiting | Drug: Linperlisib Tablet | Advanced Solid Tumor | Shanghai YingLi Pharmaceutical Co. Ltd. |
June 30, 2022 | Phase 1 |
| NCT05863871 | Not yet recruiting | Drug: Linperlisib | Focus on the Lymphoma Including B/T-cell Lymphoma |
Ruijin Hospital | May 2023 | |
| NCT05274997 | Recruiting | Drug: YY-20394 | Peripheral T/NK Cell Lymphoma (R/R PTCL) |
Shanghai YingLi Pharmaceutical Co. Ltd. |
May 1, 2022 | Phase 2 |
| NCT05676710 | Recruiting | Drug: Linperlisib | Relapsed/Refractory Large Granular T Lymphocytic Leukemia |
Institute of Hematology & Blood Diseases Hospital |
February 10, 2023 | Phase 1 |
| NCT05559008 | Recruiting | Drug: Dasatinib Drug: Linperlisib |
Peripheral T Cell Lymphoma |
Ruijin Hospital | September 30, 2022 | Phase 1 Phase 2 |
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