Cat. No.: HY-112417

Ki11502

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Ki11502 is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGF β/α receptors with IC₅₀ values less than 10 nM. Ki11502 selectively inhibits PDGF β receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Ki11502 can induce Apoptosis) and exhibits profound antiproliferative effects on select subsets of leukemia, including those with Imatinib (HY-15463) resistant mutations. Ki11502 is highly suitable for studying the role of PDGF in vascular diseases, particularly the role of proteoglycans in atherosclerosis.

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Pureté: 99.30%
CAS No.: 347155-76-4
Formule: C₂₆H₂₃N₃O₄S
Masse moléculaire:473.54

Stockage:

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

Ki11502 Chemical Structure

CAS No.: 347155-76-4

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

PDGFRα

<10 nM (IC₅₀)

PDGFRβ

<10 nM (IC₅₀)

KIT

86.81 nM (IC₅₀)

KIT670I

427.8 nM (IC₅₀)

FLT3

37.54 nM (IC₅₀)

FLT3D835Y

541.6 nM (IC₅₀)

KDR

210 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform PDGFR :

Voir tous les produits spécifiques à Isoform Akt :

Voir tous les produits spécifiques à Isoform Bcl-2 Family :

In Vitro

Ki11502 (0.1-1 nM; 2 days) significantly induces growth arrest, G0/G1 cell cycle arrest, and apoptosis in eosinophilic leukemia EOL-1 cells carrying the activated FIP1-like 1/PDGFRα fusion gene^[2].
Ki11502 (0.1-1 nM; 3 h) effectively reduces the levels of p-PDGFRα and its downstream signals (including p-Akt, p-ERK, and p-STAT5) in EOL-1 cells^[2].

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

Western Blot Analysis^[2]

Cell Line:

EOL-1, MOLM13, MV4-11
Concentration:

0.1 nM; 0.5 nM; 1 nM
Incubation Time:

48 h
Result:

Significantly downregulated the levels of Bcl-2, Bcl-xL, and Mcl-1 in EOL-1 cells, drastically reduced the level of Bcl-xL in MV4-11 cells, and notably decreased the expression of Mcl-1 in MOLM13 cells.

In Vivo

Ki11502 (50 mg/kg; gavage; twice daily for 5 consecutive days) completely inhibits the proliferation of EOL-1 tumor xenografts in SCID mice^[2].

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

Chemical Information

CAS No. 347155-76-4
Appearance Solid
Masse moléculaire 473.54
Formule C₂₆H₂₃N₃O₄S
Color White to off-white
SMILES

O=C(NC(NC1=CC=C(OC2=CC=NC3=CC(OC)=C(OC)C=C23)C=C1)=S)C4=CC=CC=C4C
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Solvant et solubilité

In Vitro:

DMSO : 16.67 mg/mL (35.20 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

2.1118 mL

10.5588 mL

21.1175 mL

5 mM

0.4224 mL

2.1118 mL

4.2235 mL

10 mM

0.2112 mL

1.0559 mL

2.1118 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 1.67 mg/mL (3.53 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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: ≥ 1.67 mg/mL (3.53 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 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 (16.7 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (274 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 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)
Instruction de manipulation (2659 KB)

Références

[1]. Getachew R, et al. Characterisation of Ki11502 as a potent inhibitor of PDGF beta receptor-mediated proteoglycan synthesis in vascular smooth muscle cells. Eur J Pharmacol. 2010;626(2-3):186-192. [Content Brief]

[2]. Nishioka C, et al. Ki11502, a novel multitargeted receptor tyrosine kinase inhibitor, induces growth arrest and apoptosis of human leukemia cells in vitro and in vivo. Blood. 2008 May 15;111(10):5086-92. [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	2.1118 mL	10.5588 mL	21.1175 mL	52.7938 mL
	5 mM	0.4224 mL	2.1118 mL	4.2235 mL	10.5588 mL
	10 mM	0.2112 mL	1.0559 mL	2.1118 mL	5.2794 mL
	15 mM	0.1408 mL	0.7039 mL	1.4078 mL	3.5196 mL
	20 mM	0.1056 mL	0.5279 mL	1.0559 mL	2.6397 mL
	25 mM	0.0845 mL	0.4224 mL	0.8447 mL	2.1118 mL
	30 mM	0.0704 mL	0.3520 mL	0.7039 mL	1.7598 mL

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Ki11502

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Voir tous les produits spécifiques à Isoform PDGFR

Voir tous les produits spécifiques à Isoform Akt

Voir tous les produits spécifiques à Isoform Bcl-2 Family

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Ki11502 Related Classifications

HY-112417 Related Classifications