Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
PI3Kδ 3.3 nM (IC50) PI3Kγ 17.9 nM (IC50) PI3Kβ 241.6 nM (IC50) PI3Kα 377.2 nM (IC50)
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ln Vitro |
PI3Kδ-IN-8 (compound 34) (0.1 nM-10 μM; 96 h), exhibits remarkable efficacy against representative DLBCL cell lines, whether they belong to the ABC subtype (OCI-Ly10 and TMD-8) or GCB (SUDHL-6)[1]. With an IC50 of 9.5 nM, PI3Kδ-IN-8 (1 h) suppresses the PI3K-induced AKT phosphorylation in anti-IgM activated Raji cells[1].
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ln Vivo |
In mice, PI3Kδ-IN-8 (1-30 mg/kg; po once daily for 24 d) significantly and dose-dependently decreases tumor weight and volume[1]. In mice, PI3Kδ-IN-8 (1 mg/kg; iv) exhibits a low clearance (5.6 mL/min/kg), an acceptable half-life (1 h), and a Cmax (2.3 μM)[1]. AUClast (22 μM·h), Cmax (7.5 μM), and moderate oral bioavailability (39%), are demonstrated by PI3Kδ-IN-8 (10 mg/kg; po) in mice[1].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: SUDHL-6, OCI-Ly10, and TMD-8 cell lines Tested Tested Concentrations: 0.1, 1, 10, 100, 1000, 10000 nM Incubation Duration: 96 hrs (hours) Experimental Results: Inhibited the viability of SUDHL-6, OCI-Ly10, and TMD-8 cells, with IC50s of <0.1 nM, <1 nM, and <0.1 nM, respectively. |
Animal Protocol |
Animal/Disease Models: Female NOD SCID (severe combined immunodeficient) mouse were injected OCI-Ly10 cells[1]
Doses: 1, 3, 10, 30 mg/kg Route of Administration: Po one time/day for 24 days Experimental Results: decreased the tumor volume, with an ED50 of 6.47 mg/kg. Tumor growth inhibition of 81.95% was seen with a highly significant reduction in both tumor volume and tumor weight. Animal/Disease Models: Male BALB/c mice[1] Doses: 1 mg/kg for iv; 10 mg/kg for po (pharmacokinetic/PK Analysis) Route of Administration: intravenous (iv) administration and oral administration Experimental Results: Iv: t1/2=1 h, Cmax =2.3 μM, CL=5.6 mL/min/kg. Po: F=39%, Cmax=7.5 μM, AUClast=22μM·h. |
References |
[1]. Shukla MR, et, al. Discovery of a Potent and Selective PI3Kδ Inhibitor (S)-2,4-Diamino-6-((1-(7-fluoro-1-(4-fluorophenyl)-4-oxo-3-phenyl-4H-quinolizin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile with Improved Pharmacokinetic Profile and Superior Efficacy i
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Molecular Formula |
C28H21F2N7O
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Molecular Weight |
509.51
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CAS # |
2101518-75-4
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C1(N)=NC(N[C@H](C2=C(C3=CC=CC=C3)C(=O)N3C(=C2C2=CC=C(F)C=C2)C=CC(F)=C3)C)=C(C#N)C(N)=N1
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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 | 1.9627 mL | 9.8134 mL | 19.6267 mL | |
5 mM | 0.3925 mL | 1.9627 mL | 3.9253 mL | |
10 mM | 0.1963 mL | 0.9813 mL | 1.9627 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.