Cat. No.: HY-13223

Crenolanib

(Synonyms: CP-868596)

17 Cited Publications

Customer Review

Based on 17 publication(s) in Google Scholar

Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with K_ds of 0.74 nM and 2.1 nM/3.2 nM, respectively.

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

Purity: 99.30%
CAS No.: 670220-88-9
Formula: C₂₆H₂₉N₅O₂
Molecular Weight:443.54

Storage:

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

Crenolanib Chemical Structure

CAS No.: 670220-88-9

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Fluorescent Dye

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (17)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

PDGFRα

2.1 nM (Kd)

PDGFRβ

3.2 nM (Kd)

FLT3

0.74 nM (Kd)

All PDGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	1.3 nM Compound: Crenolanib	Antiproliferative activity against mouse BaF3 FLT3-ITD cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 FLT3-ITD cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 32659083]
BaF3	IC₅₀	1.3 nM Compound: 25; CP-868,596	Antiproliferative activity against mouse BaF3 cells transfected with FLT3 ITD mutant assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells transfected with FLT3 ITD mutant assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 37713805]
Jurkat	IC₅₀	>1 μM Compound: Crenolanib	Cytotoxicity in human Jurkat cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay Cytotoxicity in human Jurkat cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30742435]
MOLM-13	IC₅₀	2 nM Compound: Crenolanib	Antiproliferative activity against human MOLM-13 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human MOLM-13 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 32659083]
MOLM-13	IC₅₀	2.9 nM Compound: Crenolanib	Cytotoxicity against human MOLM-13 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human MOLM-13 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay	[PMID: 32659083]
MOLM-13	IC₅₀	4.9 nM Compound: Crenolanib	Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs	[PMID: 32659083]
MOLM-13	IC₅₀	4.9 nM Compound: 18; CP-868-596	Cytotoxicity against human MOLM13 cells expressing FLT3 ITD mutant Cytotoxicity against human MOLM13 cells expressing FLT3 ITD mutant	[PMID: 31207462]
MOLM-14	IC₅₀	2 nM Compound: Crenolanib	Antiproliferative activity against human MOLM-14 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human MOLM-14 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 32659083]
MOLM-14	IC₅₀	2 nM Compound: Crenolanib	Cytotoxicity against human MOLM-14 cells assessed as reduction in cell viability incubated for 72 hrs Cytotoxicity against human MOLM-14 cells assessed as reduction in cell viability incubated for 72 hrs	[PMID: 32659083]
MV4-11	IC₅₀	0.92 nM Compound: Crenolanib	Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay	[PMID: 32659083]
MV4-11	IC₅₀	1.3 nM Compound: Crenolanib	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue assay	[PMID: 32659083]
MV4-11	IC₅₀	1.5 nM Compound: 18; CP-868-596	Cytotoxicity against human MV4-11 cells expressing FLT3 ITD mutant Cytotoxicity against human MV4-11 cells expressing FLT3 ITD mutant	[PMID: 31207462]
MV4-11	IC₅₀	12 nM Compound: Crenolanib	Cytotoxicity in human MV4-11 cells assessed as inhibition of cellular viability incubated for 72 hrs by CellTiter-Blue assay Cytotoxicity in human MV4-11 cells assessed as inhibition of cellular viability incubated for 72 hrs by CellTiter-Blue assay	[PMID: 30742435]
THP-1	IC₅₀	>1 μM Compound: Crenolanib	Cytotoxicity in human THP1 cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay Cytotoxicity in human THP1 cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30742435]

In Vitro

Crenolanib has 25-fold more affinity for PDGFRA/B compared with KIT, and is approximately 135-fold more potent than STI571 for inhibiting the PDGFRA D842V mutation. The IC₅₀ for crenolanib for a KIT exon 11 deletion mutant kinase is greater than 1,000 versus 8 nM for STI571. Crenolanib has low nanomolar potency against the V561D + D842V-mutant kinase that is similar to its potency against the isolated D842V mutation. Both STI571 and crenolanib potently inhibit the kinase activity of the fusion oncogene with IC₅₀ values of 1 and 21 nM, respectively, and inhibits PDGFRA activation in this cell line with IC₅₀ values of 93 and 26 nM, respectively^[1]. HL60/VCR and K562/ABCB1 cells, overexpressing ABCB1, are 6.9- and 3.6-fold resistant to crenolanib, respectively, in relation to parental HL60 and K562 cells. PSC-833 fully reverses resistance to crenolanib in both HL60/VCR and K562/ABCB1 cells. Crenolanib (1 nM-10 μM) stimulates ABCB1 ATPase activity in a concentration-dependent manner. Crenolanib treatment does not increase the cell surface expression of ABCB₁. Crenolanib inhibits [¹²⁵I]-IAAP photocrosslinking of ABCB1 at high concentrations, with 50 % inhibition at 10 μM, but has little effect at lower concentrations, below 1 μM^[2]. Crenolanib decreases NSCLC cell viability, induces apoptosis in NSCLC cells, and inhibits cell migration in NSCLC cells^[3].

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

In Vivo

Crenolanib (10 mg/kg and 20 mg/kg) suppresses non-small-cell lung cancer tumor growth in vivo and induces tumor cell apoptosis, and the dosage of crenolanib applied is well tolerated by recipient mice^[3].

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

Chemical Information

CAS No. 670220-88-9
Appearance Solid
Molecular Weight 443.54
Formula C₂₆H₂₉N₅O₂
Color Off-white to light yellow
SMILES

NC1CCN(C2=CC=CC3=C2N=C(N4C5=CC=C(C=C5N=C4)OCC6(COC6)C)C=C3)CC1
Synonyms

CP-868596
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Publications (17)

All Cell Imaging/StainingBio/Physico-chemical AssayWB

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Journal Impact Factor

Nature

Oncogenic fusions converge on shared mechanisms in initiating astroblastoma. [Abstract]

2025 Jul;643(8071):551-561. PMID: 40369078
Cancer Cell

Effective targeting of PDGFRA-altered high-grade glioma with avapritinib. [Abstract]

2025 Apr 14;43(4):740-756.e8. PMID: 40086436
Blood

A novel irreversible FLT3 inhibitor, FF-10101, shows excellent efficacy against AML cells with FLT3 mutations. [Abstract]

2018 Jan 25;131(4):426-438. PMID: 29187377
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
NPJ Precis Oncol

Clinical and preclinical insights into a novel MDM2::PDGFRA fusion in recurrent glioblastoma. [Abstract]

2025 Aug 16;9(1):289. PMID: 40819143
Stem Cell Res Ther

Platelet-derived growth factor (PDGF)-AA/AB in human serum are potential indicators of the proliferative capacity of human synovial mesenchymal stem cells. [Abstract]

2015 Dec 10:6:243. PMID: 26652649

Crenolanib purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2015 Dec 10:6:243. [Abstract]

Representative cell morphology. Synovial MSCs were plated at 100 cells/ cm2 and cultured for 10 days in the presence of PDGF isoforms or PDGF receptor (PDGFR) inhibitor (Crenolanib). b Fold increase of synovial MSCs. Data are shown as mean ± SD (n = 9).

Crenolanib purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2015 Dec 10:6:243. [Abstract]

Effect of exogenous platelet-derived growth factors (PDGFs) on surface markers of synovial MSCs. Synovial MSCs derived from three donors were plated at 100 cells/cm2 and cultured for 10 days in the presence of PDGF isoforms and PDGF receptor (PDGFR) inhibitor (Crenolanib).
J Med Chem

Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. [Abstract]

2019 Mar 14;62(5):2428-2446. PMID: 30742435
Glia

NG2 glia are required for maintaining microglia homeostatic state. [Abstract]

2020 Feb;68(2):345-355. PMID: 31518022

Crenolanib purchased from MedChemExpress. Usage Cited in: Glia. 2020 Feb;68(2):345-355. [Abstract]

Western blots of PDGFRα and NG2 in slices treated with CP673451 and Crenolanib for 9 days.
Mol Cancer Res

GATM-Mediated Creatine Biosynthesis Enables Maintenance of FLT3-ITD-Mutant Acute Myeloid Leukemia. [Abstract]

2022 Feb;20(2):293-304. PMID: 34635505
Br J Haematol

Comparison of effects of midostaurin, crenolanib, quizartinib, gilteritinib, sorafenib and BLU-285 on oncogenic mutants of KIT, CBL and FLT3 in haematological malignancies. [Abstract]

2019 Nov;187(4):488-501. PMID: 31309543
BMC Complement Med Ther

Baicalein alleviates fibrosis and inflammation in systemic sclerosis by regulating B-cell abnormalities. [Abstract]

2023 Feb 21;23(1):62. PMID: 36810081

Crenolanib purchased from MedChemExpress. Usage Cited in: BMC Complement Med Ther. 2023 Feb 21;23(1):62. [Abstract]

CCC-ESF-1 Cells were seeded in collagen I-coated plates and treated/not treated with TGFβ1 or PDGF in the presence or absence of Crenolanib (2 μM) for 48 h. Total collagen deposition was visualized by PSR staining.

Crenolanib purchased from MedChemExpress. Usage Cited in: BMC Complement Med Ther. 2023 Feb 21;23(1):62. [Abstract]

CCC-ESF-1 Cells were seeded in collagen I-coated plates and treated/not treated with TGFβ1 or PDGF in the presence or absence of Crenolanib (2 μM) for 48 h. Soluble collagen in the supernatant was detected by the Sircol Soluble Collagen Assay.

Crenolanib purchased from MedChemExpress. Usage Cited in: BMC Complement Med Ther. 2023 Feb 21;23(1):62. [Abstract]

CCC-ESF-1 Cells were seeded in collagen I-coated plates and treated/not treated with TGFβ1 or PDGF in the presence or absence of Crenolanib (2 μM) for 48 h. Cytotoxicity was assessed using the lactate dehydrogenase release (LDH) assay.
Anal Methods

Developing and validating a sensitive and fast UPLC-MS/MS method for estimating the in vitro metabolic stability of crenolanib in HLMs: identification of structural alarms related to the in silico toxicity and metabolic lability. [Abstract]

2025 Nov 27;17(46):9442-9453. PMID: 41246990
J Vet Med Sci

Toceranib phosphate (Palladia) reverses type 1 diabetes by preserving islet function in mice. [Abstract]

2023 Jul 17;85(7):781-789. PMID: 37258127
Hong Kong Polytechnic University

2025.
Research Square Preprint

2021 Nov.
Patent

US20200129476A1
bioRxiv

2019 Jul 1.

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (56.36 mM; ultrasonic and warming and heat to 60°C; 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

2.2546 mL

11.2729 mL

22.5459 mL

5 mM

0.4509 mL

2.2546 mL

4.5092 mL

10 mM

0.2255 mL

1.1273 mL

2.2546 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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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 90% Corn Oil

Solubility: ≥ 3 mg/mL (6.76 mM); Clear solution

This protocol yields a clear solution of ≥ 3 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 (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.43 mg/mL (3.22 mM); Clear solution

This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.43 mg/mL (3.22 mM); Clear solution

This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, 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

Protocol

Cell Assay^[2]

Viable cell numbers following drug treatment are measured using the WST-1 assay. Briefly, 1×10³ cells are seeded in 100 μL complete medium per well in 96-well tissue culture plates and incubated with crenolanib (0-10 μM) at 37°C in 5% CO₂ for 96 h. 10 μL WST-1 reagent is then added to each well, incubation is continued for two additional hours and the color developed is quantified according to the manufacturer’s instructions. Each experiment is performed in triplicate. IC₅₀ concentrations are calculated by the least square fit of dose–response inhibition in a non-linear regression model using GraphPad Prism V software.

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

Animal Administration^[3]

A549 cells are injected into the axillary regions of mice (2×10⁶ cells/mouse). When the tumor volumes reached 70 mm³, the mice are randomLy allocated to the control group, low-dose crenolanib group (10 mg/kg), or high-dose crenolanib group (20 mg/kg) (n=6 per group). The vehicle for crenolanib treatment consists of 10% 1-methyl-2-pyrrolidinone and 90% polyethylene glycol 300. The tumor size and mouse body weight are measured every other day for about 2 weeks. The tumor volume is calculated as follows: (mm³)=(width×width×length)/2. After treatment, the mice are euthanized using carbon dioxide, and the tumors are harvested and analyzed.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 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)
- 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)

References

[1]. Heinrich MC, et al.Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with STI571-resistant gastrointestinal stromal tumors. Clin Cancer Res, 2012, Jun 27. [Content Brief]

[2]. Mathias TJ, et al. The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations. Invest New Drugs. 2015 Apr;33(2):300-9. [Content Brief]

[3]. Wang P, et al. Crenolanib, a PDGFR inhibitor, suppresses lung cancer cell proliferation and inhibits tumor growth in vivo. Onco Targets Ther. 2014 Sep 26;7:1761-8. [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2546 mL	11.2729 mL	22.5459 mL	56.3647 mL
	5 mM	0.4509 mL	2.2546 mL	4.5092 mL	11.2729 mL
	10 mM	0.2255 mL	1.1273 mL	2.2546 mL	5.6365 mL
	15 mM	0.1503 mL	0.7515 mL	1.5031 mL	3.7576 mL
	20 mM	0.1127 mL	0.5636 mL	1.1273 mL	2.8182 mL
	25 mM	0.0902 mL	0.4509 mL	0.9018 mL	2.2546 mL
	30 mM	0.0752 mL	0.3758 mL	0.7515 mL	1.8788 mL
	40 mM	0.0564 mL	0.2818 mL	0.5636 mL	1.4091 mL
	50 mM	0.0451 mL	0.2255 mL	0.4509 mL	1.1273 mL

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Crenolanib

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Reprogramming Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

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Rare Diseases Drug Library

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Anti-Pulmonary Fibrosis Compound Library

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Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

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MCE Bioactive Compound Library

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Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Crenolanib

All PDGFR Isoforms

Biological Activity

Chemical Information

Publications (17)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Crenolanib Related Classifications

Cat. No.: HY-13223