Tandutinib hydrochloride (Synonyms: MLN518 hydrochloride; CT53518 hydrochloride) |
| カタログ番号GC38853 |
塩酸タンドゥチニブ (MLN518 塩酸塩) は、FLT3 の強力かつ選択的な阻害剤であり、IC50 は 0.22 μM であり、c-Kit および PDGFR もそれぞれ IC50 0.17 μM および 0.20 μM で阻害します。タンデュチニブ塩酸塩は、急性骨髄性白血病（AML）に使用できます。タンデュチニブ塩酸塩には、血液脳関門を通過する能力があります。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2438900-70-8
Sample solution is provided at 25 µL, 10mM.
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Tandutinib hydrochloride (MLN518 hydrochloride) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib hydrochloride can be used to treat acute myelogenous leukemia (AML)[1][2]. Tandutinib hydrochloride has the ability to cross the blood-brain barrier[3].
Tandutinib (0-3 μM; 30 minutes; Ba/F3 cells) treatment inhibits IL-3-independent cell growth and FLT3-ITD autophosphorylation with an IC50 of 10-100 nM in Ba/F3 cells expressing different FLT3-ITD mutants[1].Tandutinib (1 μM; 24-96 hours; Molm-14 and THP-1 AML cells) treatment induces apoptosis in FLT3-ITD-positive AML cells[1].In human FLT3-ITD-positive AML cell lines, Tandutinib inhibits FLT3-ITD phosphorylation (IC50 of ~30 nM). As with Erk2, a constitutively high level of Akt phosphorylation is readily detected and is efficiently blocked by pretreatment of the Molm-14 cells with 100-300 nM Tandutinib[1].Tandutinib inhibits cell proliferation of the FLT3-ITD-positive Molm-13 and Molm-14 with an IC50 of 10 nM. And signaling through the MAP kinase and PI3 kinase pathways[1]. Apoptosis Analysis[1] Cell Line: Molm-14 and THP-1 AML cells
Tandutinib (60 mg/kg; oral gavage; daily; for 35 days; athymic nude mice) treatment causes a statistically significant increase in survival that was extended on average by 20 days[1]. Animal Model: Athymic nude mice injected with Ba/F3 cells[1]
[1]. Kelly LM, et al. CT53518, a novel selective FLT3 antagonist for the treatment of acute myelogenous leukemia (AML). Cancer Cell. 2002 Jun;1(5):421-32. [2]. Griswold IJ, et al. Effects of MLN518, a dual FLT3 and KIT inhibitor, on normal and malignant hematopoiesis. Blood. 2004 Nov 1;104(9):2912-8. [3]. Yang JJ, et al. P-glycoprotein and breast cancer resistance protein affect disposition of tandutinib, a tyrosine kinase inhibitor. Drug Metab Lett. 2010 Dec;4(4):201-12.
| Cas No. | 2438900-70-8 | SDF | |
| 同義語 | MLN518 hydrochloride; CT53518 hydrochloride | ||
| Canonical SMILES | O=C(N1CCN(C2=C(C(C=C3OCCCN4CCCCC4)=NC=N2)C=C3OC)CC1)NC5=CC=C(OC(C)C)C=C5.Cl | ||
| Formula | C31H43ClN6O4 | M.Wt | 599.16 |
| 溶解度 | DMSO: ≥ 100 mg/mL (166.90 mM); Water: 100 mg/mL (166.90 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.669 mL | 8.345 mL | 16.69 mL |
| 5 mM | 0.3338 mL | 1.669 mL | 3.338 mL |
| 10 mM | 0.1669 mL | 0.8345 mL | 1.669 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
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