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Purity: ≥98%
PIK-90 is a novel and potent PI3Kα/γ/δ inhibitor with potential anticancer activity. It is less potent against PI3K and inhibits PI3K// with IC50s of 11 nM/18 nM/58 nM, respectively. Additionally, PIK-90 blocks DNA-PK with an IC50 of 13 nM. Studies showed that PIK-90 inhibited IgE production at doses greater than 2 mol/L while inducing increased levels of secreted IgE at 1 mol/L. According to reports, PIk-90 prevents Akt phosphorylation. It has been shown that the combination of PIK-90 and a CDK2 inhibitor causes apoptosis in LN229 PTENWT cells. Furthermore, it has been demonstrated that PIK-90 combined with siRNA directed against both CDK1 and CDK2 causes cell death, whereas PIK-90 combined with siRNA directed only against CDK1 or CDK2 had no apoptotic effect.
| Targets |
p110α (IC50 = 11 nM); p110γ (IC50 = 18 nM); p110δ (IC50 = 58 nM); p110β (IC50 = 350 nM);hsVPS34 (IC50 = 830 nM); PI3KC2β (IC50 = 64 nM ); PI3KC2α (IC50 = 47 nM); DNA-PK (IC50 = 13 nM); ATM (IC50 = 610 nM); PI4KIIIα (IC50 = 830 nM ); PI4KIIIβ (IC50 = 3.1 μM); mTORC1 (IC50 = 1.05 μM); ATR (IC50 = 15 μM)
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|---|---|
| ln Vitro |
PIK-90 shows distinct patterns of isoform selectivity to inhibit different subsets of four class I PI3K isoforms. In addition, PIK-90 completely inhibits the fMLP-stimulated phosphorylation of Akt and impairs polarity and chemotaxis in dHL60 cells. PIK-90 exhibits significantly antiproliferative activity by effectively blocking phosphorylation of Akt in six glioma cell lines varying in mutational status at PTEN or p53, including U87 MG, SF188, SF763, LN229, A1207 and LN-Z30 cells. Moreover, PIK-90 induces a modest G0G1 arrest at a concentration (0.5 μM) sufficient to inhibit phosphorylation of Akt substantially. In chronic lymphocytic leukemia (CLL) cells, PIK-90 inhibits chemotaxis to levels that are 57.8% of controls at 1 μM and 56.8% of controls at 10 μM. Pseudoemperipolesis is consistently inhibited by PIK-90 to levels that are 57.9% of controls at 10 M and 74.2% of controls at 1 M. Additionally, PIK-90 significantly lessens CXCL12-induced actin polymerization and CLL cell migration into the stromal cell layer.
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| ln Vivo |
PIK-90 (10 mg/kg) completely shields animals from this insulin-stimulated drop in blood glucose following insulin administration.
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| Enzyme Assay |
IC50 values are measured using either a standard TLC assay for lipid kinase activity or a high-throughput membrane capture assay. Kinase reactions are performed by preparing a reaction mixture containing kinase, inhibitor (2% DMSO final concentration), buffer (25 mM HEPES, pH 7.4, 10 mM MgCl2), and freshly sonicated phosphatidylinositol (100 μg/mL). Reactions are initiated by the addition of ATP containing 10 μCi of γ-32P-ATP to a final concentration 10 μM or 100 μM, and allowed to proceed for 20 minutes at room temperature. For TLC analysis, reactions are then terminated by the addition of 105 μL 1N HCl followed by 160 μL CHCl3:MeOH (1:1). The biphasic mixture is vortexed, briefly centrifuged, and the organic phase transferred to a new tube using a gel loading pipette tip precoated with CHCl3. This extract is spotted on TLC plates and developed for 3-4 hours in a 65:35 solution of n-propanol:1M acetic acid. The TLC plates are then dried, exposed to a phosphorimager screen, and quantitated. For each compound, kinase activity is typically measured at 10-12 inhibitor concentrations representing two-fold dilutions from the highest concentration tested (100 μM). For compounds showing significant activity, IC50 determinations are repeated two to four times, and the reported value is the average of these independent measurements.
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| Cell Assay |
For viabilty, cells are seeded in 12-well plates in the presence of PIK-90 for 3 days. Cell viability is determined using a WST-1 assay.
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| Animal Protocol |
FVB/N female mice are fasted at 9:00 a.m. and then given human insulin or vehicle (PBS) intravenously at 12:00 p.m.
≤10 mg/kg Administered via i.p. |
| References | |
| Additional Infomation |
N-(7,8-dimethoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)-3-pyridinecarboxamide is a member of quinazolines.
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| Molecular Formula |
C18H17N5O3
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|---|---|
| Molecular Weight |
351.37
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| Exact Mass |
351.13
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| Elemental Analysis |
C, 61.53; H, 4.88; N, 19.93; O, 13.66
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| CAS # |
677338-12-4
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| Related CAS # |
677338-12-4
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| PubChem CID |
135398491
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
817.3±65.0 °C at 760 mmHg
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| Flash Point |
448.1±34.3 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.542
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| LogP |
2.62
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
778
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NC1=NC2=C(C3=NCCN13)C=CC(OC)=C2OC)C4=CC=CN=C4
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| InChi Key |
ZJAVHOMVDCMAMF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H17N5O3/c1-25-13-6-5-12-14(15(13)26-2)21-18(23-9-8-20-16(12)23)22-17(24)11-4-3-7-19-10-11/h3-7,10H,8-9H2,1-2H3,(H,21,22,24)
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| Chemical Name |
N-(7,8-dimethoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)nicotinamide
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| Synonyms |
PIK90; PIK 90; PIK90
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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: ~0.28 mg/mL (0.8 mM)
Water: <1 mg/mL Ethanol: <1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.67 mg/mL (1.91 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 6.7 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: ≥ 0.67 mg/mL (1.91 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 6.7 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: ≥ 0.67 mg/mL (1.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1%DMSO+30% polyethylene glycol+1%Tween 80: 15mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8460 mL | 14.2300 mL | 28.4600 mL | |
| 5 mM | 0.5692 mL | 2.8460 mL | 5.6920 mL | |
| 10 mM | 0.2846 mL | 1.4230 mL | 2.8460 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 |
| NCT05917730 | Recruiting | Behavioral: Emotional Regulation and Interpersonal Abilities group Therapy (MERITA) |
Fundació Sant Joan de Déu | Domestic Violence Psychotherapy, Group Witness |
October 1, 2020 |
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