| Size | Price | Stock | Qty |
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| 25mg |
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Purity: ≥98%
Tandutinib (formerly also known as MLN-518, CT-53518, D06005, NSC726292), a piperazinyl quinazoline, is a novel, potent and selective FLT3 inhibitor/antagonist with potential antitumor activity. Its IC50 value for FLT3 inhibition is 0.22 μM. Tandutinib also inhibits c-Kit and PDGFR. It also inhibits FLT3 with a potency that is 15–20 times higher than that of CSF-1R and a selectivity that is >100 times higher than that of FGFR, EGFR, and KDR. By preventing the autophosphorylation of c-KIT, PDGF (platelet-derived growth factor) receptor tyrosine kinases, and FLT3 (FMS-Like Tyrosine kinase-3), tantutinib may have anticancer effects by preventing cell division and triggering apoptosis.
| Targets |
c-Kit (IC50 = 0.17 μM); PDGFRβ (IC50 = 0.20 μM); FLT3 (IC50 = 0.22 μM); CSF-1R (IC50 = 3.43 μM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
PDGFR family kinase autophosphorylation assays are cell-based enzyme-linked immunosorbent (ELISA) assays that use CHO cells expressing PDGFRβ wild-type, PDGFRβ/c-Kit chimeric protein, and PDGFRβ/Flt3, which contain the cytoplasmic domain of Flt-3 and c-Kit as well as the extracellular and transmembrane domains of PDGFRβ. Standard tissue culture conditions are used to grow cells to confluency in 96-well microtiter plates. After that, the cells are starved of serum for 16 hours. In summary, quiescent cells are cultured for 30 minutes at 37 °C with escalating concentrations of tantutinib, and then 8 nM PDGF-BB is added and left for 10 minutes. Lysate is obtained by centrifuging the cell lysate at 15,000g for 5 minutes after it has been lysed in 100 mM Tris, pH 7.5, 750 mM NaCl, 0.5% Triton X-100, 10 mM sodium pyrophosphate, 50 mM NaF, 10 μg/mL aprotinin, 10 μg/mL leupeptin, 1 mM phenylmethylsulfonyl fluoride, and 1 mM sodium vanadate. The lysates that have been clarified are then moved into a second microtiter plate, where the wells have been coated with 500 ng/well of 1B5B11 anti-PDGFRβ mAb and allowed to sit at room temperature for two hours. Plates are incubated at 37 °C for 60 minutes after being washed three times with binding buffer (0.3% gelatin, 25 mM HEPES, pH 7.5, 100 mM NaCl, 0.01% Tween 20). Following this, 250 ng/mL of rabbit polyclonal anti-phosphotyrosine antibody is added. Then, each well is incubated with 1 μg/mL of horseradish peroxidase-conjugated anti-rabbit antibody for 60 minutes at 37 °C after being cleaned three times with binding buffer. Before adding 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid), the wells are cleaned, and the rate of substrate formation is kept track of at 650 nm.
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| Cell Assay |
Tandutinib is exposed to cells at escalating concentrations (0.004-30 μM). Viable cells are counted after 3–7 days of cell growth in tissue culture, as assessed by Trypan blue dye exclusion. Cells are taken out, cleaned, and resuspended in 100 uL of binding buffer that has 140 mM NaCl, 2.5 mM CaCl2, and 10 mM HEPES (pH 7.4) in it every day. The cell suspension is mixed with 100 ng of annexin V-FITC and 250 ng of propidium iodide, and then it is incubated for 15 minutes at room temperature. Using a FACSort flow cytometer with an excitation wavelength of 488 nm, flow cytometry is carried out right after staining. The fluorescence of DNA propidium iodide staining and annexin V-FITC staining is measured at 585 nm and 515 nm, respectively.
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| Animal Protocol |
Female athymic nude (nu/nu) mice injected with Ba/F3 cells expressing W51 FLT3-ITD mutant
40-120 mg/kg/day Orally by gavage |
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| References |
| Molecular Formula |
C31H42N6O4
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| Molecular Weight |
562.7
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| Exact Mass |
562.33
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| Elemental Analysis |
C, 66.17; H, 7.52; N, 14.94; O, 11.37
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| CAS # |
387867-13-2
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| Related CAS # |
Tandutinib hydrochloride;2438900-70-8
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| Appearance |
Solid powder
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| SMILES |
CC(C)OC1=CC=C(C=C1)NC(=O)N2CCN(CC2)C3=NC=NC4=CC(=C(C=C43)OC)OCCCN5CCCCC5
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| InChi Key |
UXXQOJXBIDBUAC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H42N6O4/c1-23(2)41-25-10-8-24(9-11-25)34-31(38)37-17-15-36(16-18-37)30-26-20-28(39-3)29(21-27(26)32-22-33-30)40-19-7-14-35-12-5-4-6-13-35/h8-11,20-23H,4-7,12-19H2,1-3H3,(H,34,38)
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| Chemical Name |
4-[6-methoxy-7-(3-piperidin-1-ylpropoxy)quinazolin-4-yl]-N-(4-propan-2-yloxyphenyl)piperazine-1-carboxamide
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| Synonyms |
MLN 518; CT 53518; D06005; NSC726292; MLN-518; MLN0518; MLN 518; MLN518; NSC 726292; CT53518; NSC-726292; CT-53518; D-06005; D 06005; Tandutinib
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 0.5% methylcellulose: 30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7771 mL | 8.8857 mL | 17.7715 mL | |
| 5 mM | 0.3554 mL | 1.7771 mL | 3.5543 mL | |
| 10 mM | 0.1777 mL | 0.8886 mL | 1.7771 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00390468 | Completed | Drug: Tandutinib | Metastatic Cancer Pain |
National Cancer Institute (NCI) |
October 2006 | Phase 2 |
| NCT00667394 | Completed | Biological: Bevacizumab Drug: MLN-518 (Tandutinib) |
Glioblastoma Gliosarcoma |
National Cancer Institute (NCI) |
April 2008 | Phase 2 |
| NCT00408902 | Completed | Other: laboratory biomarker analysis Drug: tandutinib |
Recurrent Renal Cell Cancer Stage IV Renal Cell Cancer |
National Cancer Institute (NCI) |
November 2006 | Phase 2 |
| NCT00379080 | Completed | Drug: tandutinib Other: Tissue samples |
Adult Brain Tumor Adult Glioblastoma |
National Cancer Institute (NCI) |
January 2007 | Phase 1 Phase 2 |
| NCT00274248 | Completed | Drug: MLN518 | Acute Myelogenous Leukemia | Millennium Pharmaceuticals, Inc. | March 2005 | Phase 1 |
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