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Purity: ≥98%
PI-3065 is a novel, potent and selective inhibitor of PI3K (phosphatidylinositol 3-kinase) p110δ inhibitor with potential anticancer activity. With an IC50 of 15 nM, it blocks p110δ and exhibits >70-fold selectivity over other PI3K family proteins, including p110α, p110β, p110γ which have IC50s of 910, 600, and >10000 nM, respectively.
| Targets |
p110α (IC50 = 910 nM); p110β (IC50 = 600 nM); p110δ (IC50 = 5 nM)
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|---|---|
| ln Vitro |
PI-3065 shows no inhibition on the growth of 4T1 cells, which do not expressing detectable levels of p110δ.[1]
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| ln Vivo |
PI-3065 shows no inhibition on the growth of 4T1 cells, which do not expressing detectable levels of p110δ. [1] PI-3065 (75 mg/kg, p.o.) also inhibits the growth and metastasis of 4T1 tumors in mouse models by inactivating p110δ. PI-3065 increases survival and lowers the frequency of macroscopic metastases and other disease-related pathologies in the LSL.KrasG12D/+; p53R172H/+; PdxCretg/+ (or KPC) model of pancreatic ductal adenocarcinoma. [1]
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| Enzyme Assay |
PI-3065 is a novel, potent and selective inhibitor of PI3K (phosphatidylinositol 3-kinase) p110δ inhibitor with potential anticancer activity. It inhibitsp110δ with an IC50 of 15 nM, and showed >70-fold selectivity over other PI3K family proteins such as p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM, respectively.Cell Assay: Proliferation of 4T1 cells is assayed following a 4-h treatment with the indicated p110δ inhibitors, then washing and MTS staining are carried out after 48 h culture.PI-3065 shows no inhibition on the growth of 4T1 cells, which do not expressing detectable levels of p110δ
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| Animal Protocol |
The mammary fat pad of female WT BALB/c mice receives a 1×105 4T1 cell orthotopically inoculation on day 0. From day 1 (administered 12 hours before tumour cell inoculation), the drug (75 mg/kg PI-3065, once daily) or vehicle (0.5% methylcellulose with 0.2% Tween 80) are given orally by gavage. Weekly measurements with calipers or luminescence measurements performed on a Xenogen imaging platform are used to track tumor growth. Upon the death of the mice on day 35, tumors and ancillary organs are removed for in vitro luminescence analysis. This is done after fixation in 4% PFA and H&E staining. Prior to receiving either vehicle or PI-3065 treatment for a total of 14 days, KPC mice are allowed to develop advanced lesions measuring 5 to 10 mm (as determined by ultrasound imaging).
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| References |
| Molecular Formula |
C27H31FN6OS
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|---|---|
| Molecular Weight |
506.6380
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| Exact Mass |
506.22641
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| Elemental Analysis |
C, 64.01; H, 6.17; F, 3.75; N, 16.59; O, 3.16; S, 6.33
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| CAS # |
955977-50-1
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| Related CAS # |
955977-50-1
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| Appearance |
Solid powder
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| SMILES |
C1CC1CN2CCN(CC2)CC3=CC4=C(S3)C(=NC(=N4)C5=C(C=CC6=C5C=CN6)F)N7CCOCC7
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| InChi Key |
YDNOHCOYQVZOMC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H31FN6OS/c28-21-3-4-22-20(5-6-29-22)24(21)26-30-23-15-19(17-33-9-7-32(8-10-33)16-18-1-2-18)36-25(23)27(31-26)34-11-13-35-14-12-34/h3-6,15,18,29H,1-2,7-14,16-17H2
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| Chemical Name |
4-[6-[[4-(cyclopropylmethyl)piperazin-1-yl]methyl]-2-(5-fluoro-1H-indol-4-yl)thieno[3,2-d]pyrimidin-4-yl]morpholine
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| Synonyms |
PI 3065; PI-3065; PI3065
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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: ~50 mg/mL warming (~98.7 mM)
Water: <1 mg/mL Ethanol: <1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.93 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 (4.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9738 mL | 9.8689 mL | 19.7379 mL | |
| 5 mM | 0.3948 mL | 1.9738 mL | 3.9476 mL | |
| 10 mM | 0.1974 mL | 0.9869 mL | 1.9738 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.
Impact of pharmacological inactivation of p110δ on tumour growth and T cell responses. Nature. 2014, 510(7505), 407-411. |
Characterisation of the p110δ-selective inhibitor PI-3065 |
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