2. Protein Tyrosine Kinase/RTK Apoptosis PI3K/Akt/mTOR Cell Cycle/DNA Damage
  3. PDGFR FLT3 Apoptosis Akt PERK Bcl-2 Family
  4. Ki11502

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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Ki11502 Chemical Structure

Ki11502 Chemical Structure

CAS No. : 347155-76-4

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Based on 1 publication(s) in Google Scholar

Ki11502 Related Antibodies

Top Publications Citing Use of Products

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PDGFR PDGFRβ PDGFRα

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Akt Akt1 Akt2 Akt3

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

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  • Purity & Documentation

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Description

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[1][2].

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)

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.

Ki11502 Related Antibodies

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.
Molecular Weight

473.54

Formula

C26H23N3O4S
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1118 mL 10.5588 mL 21.1175 mL
5 mM 0.4224 mL 2.1118 mL 4.2235 mL
View the 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.

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

Mass
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
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 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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ki11502347155-76-4Ki 11502Ki-11502PDGFRFLT3ApoptosisAktPERKBcl-2 FamilyPlatelet-derived growth factor receptorCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3PKBProtein kinase BProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseVascular smooth muscle cellvascular diseasesatherosclerosisEOL-1MOLM13MV4-11SCID miceleukemiaInhibitorinhibitorinhibit

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