| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PROTAC PI3Kδ degrader-1 (compound B14) (0.001-10 μM, 72 h) exhibited potent antiproliferative activity against SU-DHL-6 and Pfeiffer cells (GI50 of 0.17 and 0.35 μM, respectively) [1]. PROTAC PI3Kδ degrader-1 (10 mM, 0-48 h) showed excellent stability, with 80% remaining after 48 h of incubation [1]. PROTAC PI3Kδ degrader-1 (0.1-1 μM, 6-24 h) degraded p-AKT and p110δ (DC50: 3.98 nM) in SU-DHL-6 cells in a dose- and time-dependent manner [1]. PROTAC PI3Kδ (1-100 nM, 24 h) degrader-1 increased the LC3II/LC3I ratio, thereby initiating autophagy in SU-DHL-6 cells [1]. PROTAC PI3Kδ degrader-1 (0.1-1 μM, 12 h) has a stronger binding affinity for VHL ligase ligands, p110δ and p-AKT, and the antiproliferative activity of its two derivatives is weaker than that of itself (GI50: 0.17 μM vs 0.90 μM and 0.87 μM)[1]. PROTAC PI3Kδ degrader-1 (100 nM, 12 h) degrades p110δ in SU-DHL-6 cells via the ubiquitin-proteasome pathway, while MLN4924 (ubiquitination inhibitor) and MG132 (proteasome inhibitor) can reverse this effect[1]. PROTAC PI3Kδ degrader-1 selectively inhibits PI3Kδ (IC50: 8 nM) and has >70-fold selectivity for the other three isoforms in SU-DHL-6 cells (IC50 >589 nM)[1]. PROTAC PI3Kδ degrader-1 (1-1000 nM, 24 h) has a strong degradative effect on p110δ, but a weak effect on p110α and p110β protein levels (DC50 > 1000 nM), and no degradative effect on p110γ in SU-DHL-6 cells [1]. PROTAC PI3Kδ degrader-1 (0.01-1 μM, 24 h) increases the proportion of G1 phase cells in SU-DHL-6 cells in a dose-dependent manner and significantly induces cell death and damage [1].
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| ln Vivo |
PROTAC PI3Kδ degrader-1 (compound B14) (2-10 mg/kg, intraperitoneal injection, once every 2 days for 21 days) showed significant antitumor efficacy in SU-DHL-6 xenograft mouse model with no obvious toxicity [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: SU-DHL-6 cells Tested Concentrations: 0.1, 1, 3, 10, 30, 100, 1000 nM Incubation Duration: 24 hours Experimental Results: At concentrations of 100 nM and 1000 nM, the protein levels of p110δ and p-AKT were effectively degraded. The degradation of p110δ was induced in a concentration-dependent manner, and the level of p-AKT was correspondingly reduced. The LC3II/LC3I ratio was increased, and autophagy was initiated. At concentrations of 100 nM and 1000 nM, the degradation rates of p110δ reached 58% and 65%, respectively, demonstrating highly efficient p110δ degradation activity. Cell cycle analysis [1] Cell Types: SU-DHL-6 cells Tested Concentrations: 0.01, 0.1, 1 μM Incubation Duration: 24 hours Experimental Results: Dose-dependently increased the proportion of cells in the G1 phase. Compared with 10 μM Idelalisib, 0.1 μM Idelalisib induced cell cycle arrest more effectively. Apoptosis analysis [1] Cell Types: SU-DHL-6 cells Tested Concentrations: 0.01, 0.1, 1 μM Incubation Duration: 24 hours Experimental Results: induced a large number of cell deaths and damage. Compared with the same dose of Idelalisib, the induced apoptosis rate was higher. |
| Animal Protocol |
Animal/Disease Models:SU-DHL-6 cells (1×10⁷ cells/mouse) were subcutaneously injected into male Balb/c nude mice aged 4–6 weeks [1].
Doses: 2, 10 mg/kg. Route of Administration: Intraperitoneal injection every 2 days for 21 days, followed by measurement of tumor size and body weight. Experimental Results: SU-DHL-6 cells showed significant antitumor activity, with tumor growth inhibition rates of 59.1% and 73.3% at doses of 2 mg/kg and 10 mg/kg, respectively. No significant toxicity was observed at the 10 mg/kg dose, and no significant changes in body weight or death were observed. SU-DHL-6 cells significantly reduced p110δ protein levels and dose-dependently reduced p-AKT expression. SU-DHL-6 cell proliferation activity was significantly reduced, and Ki67 levels were also significantly reduced. No obvious organ damage was caused; the heart, liver, spleen, and kidney tissues were morphologically normal. |
| References |
| Molecular Formula |
C63H79N11O8S
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|---|---|
| Molecular Weight |
1150.44
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C([C@@H](NC(CCCCCCCCCN1CCC(C(N2CC[C@H](NC3=NC=NC4=CC=C(C5=CN=C(C(C(OC6=CC=CC=C6)=O)=C5)OC)N=C43)C2)=O)CC1)=O)C(C)(C)C)N7[C@@H](C[C@H](C7)O)C(N[C@H](C8=CC=C(C=C8)C9=C(N=CS9)C)C)=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 | 0.8692 mL | 4.3462 mL | 8.6923 mL | |
| 5 mM | 0.1738 mL | 0.8692 mL | 1.7385 mL | |
| 10 mM | 0.0869 mL | 0.4346 mL | 0.8692 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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