Art. -Nr.: HY-120265

MIPS-9922

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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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Reinheit: 99.25%
CAS. Nr.: 1416956-33-6
Formel: C₂₈H₃₁F₂N₉O₂
Molecular Weight:563.60

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

MIPS-9922 Chemical Structure

CAS. Nr.: 1416956-33-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PI3Kβ

63 nM (IC₅₀)

PI3Kδ

2200 nM (IC₅₀)

Alle PI3K Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-468	EC₅₀	4.6 μM Compound: 21	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	[PMID: 23795239]
MDA-MB-468	IC₅₀	<10 nM Compound: 21	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	[PMID: 23795239]
Sf21	IC₅₀	8100 nM Compound: 21	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	[PMID: 23795239]
Sf21	IC₅₀	6 μM Compound: 21	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	[PMID: 23795239]

In Vitro

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.

In Vivo

MIPS-9922 (2.5 mg/kg, bolus jugular vein injection; once) prevents arterial thrombus formation in the in vivo electrolytic mouse model of thrombosis without inducing prolonged bleeding or excess blood loss^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male C57BL/6 mice bearing electrolytic injury^[1]
Dosage:

2.5 mg/kg
Administration:

Bolus jugular vein injection; once
Result:

Prevented arterial thrombus formation in the in vivo electrolytic mouse model of thrombosis.

Chemical Information

CAS. Nr. 1416956-33-6
Appearance Solid
Molecular Weight 563.60
Formel C₂₈H₃₁F₂N₉O₂
Color White to off-white
SMILES

O=C(N1CCN(C2=NC(N3C4=CC=CC=C4N=C3C(F)F)=NC(N5CCOCC5)=N2)CC1)[C@@H](N)CC6=CC=CC=C6
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7743 mL

8.8715 mL

17.7431 mL

5 mM

0.3549 mL

1.7743 mL

3.5486 mL

10 mM

0.1774 mL

0.8872 mL

1.7743 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhaohua Zheng, et al. Discovery and antiplatelet activity of a selective PI3Kβ inhibitor (MIPS-9922). Eur J Med Chem. 2016 Oct 21:122:339-351. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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MIPS-9922

MCE Bioactive Compound Library

Alle PI3K Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MIPS-9922 Related Classifications

HY-120265 Related Classifications