Lestaurtinib
Based on 4 publication(s) in Google Scholar
Lestaurtinib (CEP-701) is an orally active and selective RPTKs (receptor protein tyrosine kinase) inhibitor, competitively inhibits ATP binding to the TrkA/B/C domain. Lestaurtinib inhibits RPTKs phosphorylation, with IC50s of 2, 25 and 0.9 nM for FLT3, TrkA and JAK2, respectively. Lestaurtinib induces apoptosis and cycle arrest, also can inhibit growth of tumor.
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- Pureza: 99.66%
- No. CAS: 111358-88-4
- Fòrmula: C26H21N3O4
- Peso molecular:439.46
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Almacenamiento:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Lestaurtinib
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Actividad biológica
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JAK2 0.9 nM (IC50) |
TrkA 25 nM (IC50) |
FLT3 2 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
32 nM
Compound: CEP-701
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Toxicity against human A375 cells after 72 hrs by cell titer-blue assay
Toxicity against human A375 cells after 72 hrs by cell titer-blue assay
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[PMID: 19654408] |
| BaF3 | GI50 |
<200 nM
Compound: 2
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Growth inhibition of mouse Baf3 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Growth inhibition of mouse Baf3 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
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[PMID: 35923716] |
| BaF3 | GI50 |
5 nM
Compound: 2
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Growth inhibition of mouse BAF3 cells harboring FLT3 ITD mutant assessed as reduction in cell inhibition measured after 72 hrs by MTT assay
Growth inhibition of mouse BAF3 cells harboring FLT3 ITD mutant assessed as reduction in cell inhibition measured after 72 hrs by MTT assay
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[PMID: 35923716] |
| BaF3 | IC50 |
3 nM
Compound: Lestaurtinib
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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 |
5 nM
Compound: Lestaurtinib
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Antiproliferative activity against mouse BaF3 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 mouse BaF3 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] |
| BFTC-905 | CC50 |
>3 μM
Compound: 46; CEP-701, KT-5555
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Cytotoxicity against human BFTC-905 cells
Cytotoxicity against human BFTC-905 cells
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[PMID: 33539089] |
| MV4-11 | GI50 |
33 nM
Compound: Lestaurtinib
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Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition after 72 hrs by WST assay
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition after 72 hrs by WST assay
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[PMID: 32272419] |
| MV4-11 | IC50 |
0.009 μM
Compound: Lestaurtinib
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Antiproliferative activity against wild type FLT3 expressing human MV411 cells after 72 hrs by WST8 assay
Antiproliferative activity against wild type FLT3 expressing human MV411 cells after 72 hrs by WST8 assay
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[PMID: 20153646] |
| MV4-11 | IC50 |
2.1 nM
Compound: CEP-701
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Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay
Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay
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[PMID: 19654408] |
| MV4-11 | IC50 |
2.5 nM
Compound: 3
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Inhibition of FLT3-mediated STAT5 phosphorylation in human MV411 cells after 1 hr by immunoblotting analysis
Inhibition of FLT3-mediated STAT5 phosphorylation in human MV411 cells after 1 hr by immunoblotting analysis
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10.1039/C1MD00175B |
| RS4-11 | IC50 |
0.12 μM
Compound: Lestaurtinib
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Antiproliferative activity against human RS4:11 cells having FLT3-ITD mutation after 72 hrs by WST8 assay
Antiproliferative activity against human RS4:11 cells having FLT3-ITD mutation after 72 hrs by WST8 assay
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[PMID: 20153646] |
| RS4-11 | IC50 |
1.5 nM
Compound: CEP-701
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Inhibition of FLT3 ITD mutant autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
Inhibition of FLT3 ITD mutant autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
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[PMID: 19654408] |
| RS4-11 | IC50 |
2.6 nM
Compound: CEP-701
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Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
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[PMID: 19654408] |
Lestaurtinib (0.01-10 μM; 72 h) inhibits growth of ATC cells, with IC50s of 0.21, 0.41 and 2.35 μM for KMH2, CAL62 and THJ-21T cells, respectively[1].
Lestaurtinib (0.125-4 μM; 24 h) decreases STAT5 phosphorylation in a concentration-dependent manner, and completely inhibits expression of pSTAT5 at 4 μM[1].
Lestaurtinib (0.5 μM; 24 h) shows antiproliferative effect on WI-38, CAL62 and KMH2 cells[1].
Lestaurtinib (4 μM; 24 h) induces cell cycle arrest in the G2/M phase in CAL62 and KMH2 cells[1].
Lestaurtinib (30-300 nM; 48 h) induces apoptosis in a dose-dependent manner in HL (hodgkin lymphoma) cell lines[2].
Lestaurtinib (30, 100, 300 nM; 1 h) inhibits JAK2, STAT5 and STAT3 phosphorylation when at 300 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KMH2, CAL62, THJ-21T cells
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Concentration:0.01-10 µM
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Incubation Time:72 h
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Result:Showed good growth inhibitory activity with IC50s of 0.21, 0.41 and 2.35 µM for KMH2, CAL62 and THJ-21T cells, respectively.
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Cell Line:WI-38, CAL62 and KMH2 cells
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Concentration:0.5 µM
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Incubation Time:24 h
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Result:Inhibited proliferation of ATC cells.
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Cell Line:CAL62 and KMH2 cells
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Concentration:4 μM
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Incubation Time:24 h
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Result:Led to increase in the number of cells in the G2/M phase, and decrease in the number of cells in the G1/G0 and S phases (KMH2 cells more significant than CAL62 cells).
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Cell Line:CAL62 cells
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Concentration:0.125-4 µM
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Incubation Time:24 h
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Result:Decreased pSTAT5 in a concentration-dependent manner, with a complete disappearance of pSTAT5expression at 4 μM.
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Cell Line:L-428, L-1236, L-540, HDLM-2 and HDMY-Z cells
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Concentration:30-300 nM
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Incubation Time:48 h
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Result:Increased apoptosis rate of 62%, 57%, 10%, 64%, 30% for L-428, L-1236, L-540, HDLM-2 and HD-MY-Z cells respectively, when at 300 nM (in a dose-dependent manner).
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Cell Line:L-428, L-1236, L-540, HDLM-2 and HD-MY-Z cells
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Concentration:30, 100, 300 nM
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Incubation Time:1 h
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Result:Decreased phospho-JAK2, -STAT5 and -STAT3 levels of all the HL cell lines by 46-94%, 88-100% and 97-100%, respectively (when at 300 nM).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Four-week-old athymic nu/nu mice (SY5Y-TrkB xenografts model)[3].
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Dosage:20 mg/kg
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Administration:Subcutaneous injection; twice daily (monday to friday) and once daily (saturday and sunday); 3 weeks.
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Result:Significantly slowed the growth of SY5Y-TrkB xenografts.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 111358-88-4
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Appearance Solid
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Peso molecular 439.46
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Fòrmula C26H21N3O4
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Color White to off-white
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SMILES
O=C(NC1)C2=C1C3=C(C4=C52)N(C6=C3C=CC=C6)[C@@]([C@@](O)(CO)C7)(C)O[C@H]7N4C8=C5C=CC=C8
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Synonyms
CEP-701; KT-5555
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (4)
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Journal Impact Factor
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Most Recent
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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 -
Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929 -
Cancer Cell Int
Construction of a prognostic model with histone modification-related genes and identification of potential drugs in pancreatic cancer. [Abstract]2021 Jun 5;21(1):291. PMID: 34090418 -
bioRxiv
Sphingosine-1-phosphate receptor modulators resensitize FLT3-ITD acute myeloid leukemia cells with NRAS mutations to FLT3 inhibitors. [Abstract]2025 Nov 24:2025.11.21.689510. PMID: 41341164
Solvente y solubilidad
DMSO : 50 mg/mL (113.78 mM; Need ultrasonic; 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.08 mg/mL (4.73 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.73 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Pureza y Documentación
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Ficha de datos (296 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Pinto N, et al. Lestaurtinib is a potent inhibitor of anaplastic thyroid cancer cell line models. PLoS One. 2018 Nov 12;13(11):e0207152. [Content Brief]
[2]. Diaz T, et al. Lestaurtinib inhibition of the Jak/STAT signaling pathway in hodgkin lymphoma inhibits proliferation and induces apoptosis. PLoS One. 2011 Apr 20;6(4):e18856. [Content Brief]
[3]. Iyer R, et al. Lestaurtinib enhances the antitumor efficacy of chemotherapy in murine xenograft models of neuroblastoma. Clin Cancer Res. 2010 Mar 1;16(5):1478-85. [Content Brief]
[4]. Levis M, et al. A FLT3-targeted tyrosine kinase inhibitor is cytotoxic to leukemia cells in vitro and in vivo. Blood. 2002 Jun 1;99(11):3885-91. [Content Brief]
[5]. Shabbir M, et al. Lestaurtinib, a multitargeted tyrosine kinase inhibitor: from bench to bedside. Expert Opin Investig Drugs. 2010 Mar;19(3):427-36. [Content Brief]
[6]. Hexner EO, et al. Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders. Blood. 2008 Jun 15;111(12):5663-71. [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, 6 months; -20°C, 1 month (protect from light). 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 | 2.2755 mL | 11.3776 mL | 22.7552 mL | 56.8880 mL |
| 5 mM | 0.4551 mL | 2.2755 mL | 4.5510 mL | 11.3776 mL | |
| 10 mM | 0.2276 mL | 1.1378 mL | 2.2755 mL | 5.6888 mL | |
| 15 mM | 0.1517 mL | 0.7585 mL | 1.5170 mL | 3.7925 mL | |
| 20 mM | 0.1138 mL | 0.5689 mL | 1.1378 mL | 2.8444 mL | |
| 25 mM | 0.0910 mL | 0.4551 mL | 0.9102 mL | 2.2755 mL | |
| 30 mM | 0.0759 mL | 0.3793 mL | 0.7585 mL | 1.8963 mL | |
| 40 mM | 0.0569 mL | 0.2844 mL | 0.5689 mL | 1.4222 mL | |
| 50 mM | 0.0455 mL | 0.2276 mL | 0.4551 mL | 1.1378 mL | |
| 60 mM | 0.0379 mL | 0.1896 mL | 0.3793 mL | 0.9481 mL | |
| 80 mM | 0.0284 mL | 0.1422 mL | 0.2844 mL | 0.7111 mL | |
| 100 mM | 0.0228 mL | 0.1138 mL | 0.2276 mL | 0.5689 mL |
Lestaurtinib Related Classifications
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