Crenolanib
Based on 18 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 Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.30%
- No. CAS: 670220-88-9
- Fòrmula: C26H29N5O2
- Peso molecular:443.54
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Crenolanib
More- Nature. 2025 Jul;643(8071):551-561. [Abstract]
- Cancer Cell. 2025 Apr 14;43(4):740-756.e8. [Abstract]
- Blood. 2018 Jan 25;131(4):426-438. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Cell Rep Med. 2026 Jun 25:102886. [Abstract]
- NPJ Precis Oncol. 2025 Aug 16;9(1):289. [Abstract]
- Stem Cell Res Ther. 2015 Dec 10:6:243. [Abstract]
- J Med Chem. 2019 Mar 14;62(5):2428-2446. [Abstract]
- Mol Cancer Res. 2022 Feb;20(2):293-304. [Abstract]
- Glia. 2020 Feb;68(2):345-355. [Abstract]
- BMC Complement Med Ther. 2023 Feb 21;23(1):62. [Abstract]
- Br J Haematol. 2019 Nov;187(4):488-501. [Abstract]
- Anal Methods. 2025 Nov 27;17(46):9442-9453. [Abstract]
- J Vet Med Sci. 2023 Jul 17;85(7):781-789. [Abstract]
- Hong Kong Polytechnic University. 2025.
- Research Square Preprint. 2021 Nov.
- Patent. US20200129476A1
- bioRxiv. 2019 Jul 1.
Customer Validation & Images
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Cell Imaging/Staining
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
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WB
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Cell Imaging/Staining
Actividad biológica
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PDGFRα 2.1 nM (Kd) |
PDGFRβ 3.2 nM (Kd) |
FLT3 0.74 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
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| BaF3 | IC50 |
1.3 nM
Compound: Crenolanib
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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
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[PMID: 32659083] |
| BaF3 | IC50 |
1.3 nM
Compound: 25; CP-868,596
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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
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[PMID: 37713805] |
| Jurkat | IC50 |
>1 μM
Compound: Crenolanib
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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
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[PMID: 30742435] |
| MOLM-13 | IC50 |
2 nM
Compound: Crenolanib
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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
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[PMID: 32659083] |
| MOLM-13 | IC50 |
2.9 nM
Compound: Crenolanib
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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
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[PMID: 32659083] |
| MOLM-13 | IC50 |
4.9 nM
Compound: Crenolanib
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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
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[PMID: 32659083] |
| MOLM-13 | IC50 |
4.9 nM
Compound: 18; CP-868-596
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Cytotoxicity against human MOLM13 cells expressing FLT3 ITD mutant
Cytotoxicity against human MOLM13 cells expressing FLT3 ITD mutant
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[PMID: 31207462] |
| MOLM-14 | IC50 |
2 nM
Compound: Crenolanib
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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
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[PMID: 32659083] |
| MOLM-14 | IC50 |
2 nM
Compound: Crenolanib
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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
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[PMID: 32659083] |
| MV4-11 | IC50 |
0.92 nM
Compound: Crenolanib
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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
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[PMID: 32659083] |
| MV4-11 | IC50 |
1.3 nM
Compound: Crenolanib
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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
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[PMID: 32659083] |
| MV4-11 | IC50 |
1.5 nM
Compound: 18; CP-868-596
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Cytotoxicity against human MV4-11 cells expressing FLT3 ITD mutant
Cytotoxicity against human MV4-11 cells expressing FLT3 ITD mutant
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[PMID: 31207462] |
| MV4-11 | IC50 |
12 nM
Compound: Crenolanib
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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
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[PMID: 30742435] |
| THP-1 | IC50 |
>1 μM
Compound: Crenolanib
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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
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[PMID: 30742435] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 670220-88-9
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Appearance Solid
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Peso molecular 443.54
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Fòrmula C26H29N5O2
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Color Off-white to light yellow
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SMILES
NC1CCN(C2=CC=CC3=C2N=C(N4C5=CC=C(C=C5N=C4)OCC6(COC6)C)C=C3)CC1
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Synonyms
CP-868596
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (18)
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Journal Impact Factor
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Most Recent
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Nature
2025 Jul;643(8071):551-561. PMID: 40369078 -
Cancer Cell
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 -
Cell Rep Med
GPNMB+ macrophages promote osteogenic differentiation of nucleus pulposus cells through PDGF signaling in intervertebral disc degeneration. [Abstract]2026 Jun 25:102886. PMID: 42349413 -
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).
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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 -
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 -
Glia
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.
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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.
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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 -
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 -
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Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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.
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.
Pureza y Documentación
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Ficha de datos (283 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
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, 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 |
Crenolanib Related Classifications
HY-13223 Related Classifications
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