MIPS-9922
Based on 1 Customer Validation
MIPS-9922 is a potent and selective PI3Kβ inhibitor with an IC50 of 63 nM. MIPS-9922 inhibits PI3Kβ with >30-fold higher potency than PI3Kδ. MIPS-9922 blocks PI3K mediated activation of platelet glycoprotein αIIbβ3 activation and platelet adhesion in vitro. MIPS-9922 shows anti-platelet and anti-thrombotic activities.
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- Purity: 99.25%
- CAS No.: 1416956-33-6
- 화학식: C28H31F2N9O2
- 분자량:563.60
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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PI3Kβ 63 nM (IC50) |
PI3Kδ 2200 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-468 | EC50 |
4.6 μM
Compound: 21
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Cytotoxicity against PTEN-deficient human MDA-MB-468 cells assessed as inhibition of cell growth after 48 hrs by Cell Titer 96 assay
Cytotoxicity against PTEN-deficient human MDA-MB-468 cells assessed as inhibition of cell growth after 48 hrs by Cell Titer 96 assay
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[PMID: 23795239] |
| MDA-MB-468 | IC50 |
<10 nM
Compound: 21
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Inhibition of IGF-1 induced Akt phosphorylation in PTEN-deficient human MDA-MB-468 cells pretreated for 2 hrs before IGF1 induction measured after 15 mins by Western blot analysis
Inhibition of IGF-1 induced Akt phosphorylation in PTEN-deficient human MDA-MB-468 cells pretreated for 2 hrs before IGF1 induction measured after 15 mins by Western blot analysis
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[PMID: 23795239] |
| Sf21 | IC50 |
8100 nM
Compound: 21
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Inhibition of recombinant PI3K-alpha Q589D mutant (unknown origin) expressed in baculovirus infected Sf21 cells assessed as decrease in ATP consumption using phosphatidylinositol bisphosphate and 100 uM ATP as substrate measured after 60 mins by luminesce
Inhibition of recombinant PI3K-alpha Q589D mutant (unknown origin) expressed in baculovirus infected Sf21 cells assessed as decrease in ATP consumption using phosphatidylinositol bisphosphate and 100 uM ATP as substrate measured after 60 mins by luminesce
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[PMID: 23795239] |
| Sf21 | IC50 |
6 μM
Compound: 21
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Inhibition of recombinant PI3K-beta D862Q mutant (unknown origin) expressed in baculovirus infected Sf21 cells assessed as decrease in ATP consumption using phosphatidylinositol bisphosphate and 100 uM ATP as substrate measured after 60 mins by luminescen
Inhibition of recombinant PI3K-beta D862Q mutant (unknown origin) expressed in baculovirus infected Sf21 cells assessed as decrease in ATP consumption using phosphatidylinositol bisphosphate and 100 uM ATP as substrate measured after 60 mins by luminescen
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[PMID: 23795239] |
MIPS-9922 potently inhibits ADP-induced washed platelet aggregation. MIPS-9922 also inhibits integrin αIIbβ3 activation and αIIbβ3 dependent platelet adhesion to immobilized von Willebrand Factor (vWF) under high shear[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice bearing electrolytic injury[1]
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Dosage:2.5 mg/kg
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Administration:Bolus jugular vein injection; once
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Result:Prevented arterial thrombus formation in the in vivo electrolytic mouse model of thrombosis.
Chemical Information
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CAS No. 1416956-33-6
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Appearance Solid
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분자량 563.60
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화학식 C28H31F2N9O2
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Color White to off-white
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SMILES
O=C(N1CCN(C2=NC(N3C4=CC=CC=C4N=C3C(F)F)=NC(N5CCOCC5)=N2)CC1)[C@@H](N)CC6=CC=CC=C6
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (177.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7743 mL | 8.8715 mL | 17.7431 mL | 44.3577 mL |
| 5 mM | 0.3549 mL | 1.7743 mL | 3.5486 mL | 8.8715 mL | |
| 10 mM | 0.1774 mL | 0.8872 mL | 1.7743 mL | 4.4358 mL | |
| 15 mM | 0.1183 mL | 0.5914 mL | 1.1829 mL | 2.9572 mL | |
| 20 mM | 0.0887 mL | 0.4436 mL | 0.8872 mL | 2.2179 mL | |
| 25 mM | 0.0710 mL | 0.3549 mL | 0.7097 mL | 1.7743 mL | |
| 30 mM | 0.0591 mL | 0.2957 mL | 0.5914 mL | 1.4786 mL | |
| 40 mM | 0.0444 mL | 0.2218 mL | 0.4436 mL | 1.1089 mL | |
| 50 mM | 0.0355 mL | 0.1774 mL | 0.3549 mL | 0.8872 mL | |
| 60 mM | 0.0296 mL | 0.1479 mL | 0.2957 mL | 0.7393 mL | |
| 80 mM | 0.0222 mL | 0.1109 mL | 0.2218 mL | 0.5545 mL | |
| 100 mM | 0.0177 mL | 0.0887 mL | 0.1774 mL | 0.4436 mL |
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