PDGFRα kinase inhibitor 1

Name: PDGFRα kinase inhibitor 1
Brand: MedChemExpress
SKU: HY-111507
Rating: 4.5 (1 reviews)

Cat. No.: HY-111507 Purity: 99.78%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC₅₀s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively.

For research use only. We do not sell to patients.

PDGFRα kinase inhibitor 1 Chemical Structure

CAS No. : 2209053-93-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 452	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 452	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 990	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1650	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2500	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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PDGFR PDGFRβ PDGFRα

Biological Activity
Purity & Documentation
References
Customer Review

Description

PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC₅₀s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively^[1].

IC₅₀ & Target^[1]

PDGFRα

132 nM (IC₅₀)

PDGFRβ

6115 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	> 10 μM Compound: 15i	Cytotoxicity against mouse BA/F3 cells after 72 hrs by CellTiter-Glo or CCK-8 assay Cytotoxicity against mouse BA/F3 cells after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 29544149]
EOL1	GI₅₀	< 0.001 μM Compound: 15i	Antiproliferative activity against human EOL-1 cells after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human EOL-1 cells after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 29544149]
NCI-H1703	GI₅₀	2.99 μM Compound: 15i	Antiproliferative activity against human NCI-H1703 cells after 72 hrs in presence of PDGF-AA by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human NCI-H1703 cells after 72 hrs in presence of PDGF-AA by CellTiter-Glo or CCK-8 assay	[PMID: 29544149]
NCI-H1703	GI₅₀	5.37 μM Compound: 15i	Antiproliferative activity against human NCI-H1703 cells after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human NCI-H1703 cells after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 29544149]

In Vitro

PDGFRα kinase inhibitor 1 (CHMFL-PDGFR-159, Compound 15i) exhibits weak inhibition to DDR1 kinase (IC₅₀: 2462±126 nM)^[1].

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

Molecular Weight

586.69

Formula

C₃₄H₃₄N₈O₂

CAS No.

2209053-93-8

Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C=CC(NC(C1=CC=C(CN(CCN(C)C)C(C2=CC=CN=C2)=O)C=C1)=O)=C3)=C3NC4=NC=CC(C5=CC=CN=C5)=N4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 260 mg/mL (443.16 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	1.7045 mL	8.5224 mL	17.0448 mL
5 mM	0.3409 mL	1.7045 mL	3.4090 mL
10 mM	0.1704 mL	0.8522 mL	1.7045 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 2.17 mg/mL (3.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.17 mg/mL (3.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.17 mg/mL (3.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 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 (21.7 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

Animal weight
(per animal)

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

Purity: 99.78%

Select Batch:

Data Sheet (272 KB) SDS (252 KB)

COA (248 KB) LCMS (269 KB)

Handling Instructions (2659 KB)

References

[1]. Wang Q, et al. Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophi [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7045 mL	8.5224 mL	17.0448 mL	42.6119 mL
	5 mM	0.3409 mL	1.7045 mL	3.4090 mL	8.5224 mL
	10 mM	0.1704 mL	0.8522 mL	1.7045 mL	4.2612 mL
	15 mM	0.1136 mL	0.5682 mL	1.1363 mL	2.8408 mL
	20 mM	0.0852 mL	0.4261 mL	0.8522 mL	2.1306 mL
	25 mM	0.0682 mL	0.3409 mL	0.6818 mL	1.7045 mL
	30 mM	0.0568 mL	0.2841 mL	0.5682 mL	1.4204 mL
	40 mM	0.0426 mL	0.2131 mL	0.4261 mL	1.0653 mL
	50 mM	0.0341 mL	0.1704 mL	0.3409 mL	0.8522 mL
	60 mM	0.0284 mL	0.1420 mL	0.2841 mL	0.7102 mL
	80 mM	0.0213 mL	0.1065 mL	0.2131 mL	0.5326 mL
	100 mM	0.0170 mL	0.0852 mL	0.1704 mL	0.4261 mL