Tandutinib (MLN518)
4-[6-Methoxy-7-(3-piperidin-1-ylpropoxy)quinazolin-4-yl]-N-(4-propan-2-yloxyphenyl)piperazine-1-carboxamide
CAS: 387867-13-2
Molecular Formula: C31H42N6O4
Tandutinib (MLN518) - Names and Identifiers
Tandutinib (MLN518) - Physico-chemical Properties
| Molecular Formula | C31H42N6O4 |
| Molar Mass | 562.7 |
| Density | 1.213±0.06 g/cm3(Predicted) |
| Melting Point | 177-178°C |
| Boling Point | 769.5±60.0 °C(Predicted) |
| Flash Point | 419.2°C |
| Solubility | Chloroform (Slightly), Methanol (Slightly) |
| Vapor Presure | 1.35E-23mmHg at 25°C |
| Appearance | Solid |
| Color | White to Off-White |
| pKa | 13.39±0.70(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| Refractive Index | 1.61 |
| Use | Tandutinib (MLN518) is an effective FLT3 antagonist with an IC50 of 0.22 μM. It also inhibits PDGFR and c-Kit. Its effect on FLT3 is 15 to 20 times stronger than CSF-1R and more than 100 times stronger than FGFR, EGFR and KDR. |
| In vitro study | Unlike Staurosporin, Tandutinib effectively inhibits the autophosphorylation of FLT3, βpdgf and c-Kit with an IC50 of 0.17-0.22 μm, while it acts on EGFR, FGFR, KDR, InsR, Src, Abl, PKC, PKA, and MAPKs have little effect. Tandutinib inhibits IL-3-independent cell growth and also inhibits FLT3-ITD autophosphorylation with an IC50 of 10-100 nM. Tandutinib also inhibited the proliferation of human leukemia Ba/F3 cells containing the FLT3-ITD mutation with an IC50 of 10-30 nM and inhibited FLT3-ITD-positive Molm-13 and Molm-14 cells with an IC50 of 10 nM. Tandutinib acted on FLT3-ITD-positive Molm-14 cells but not FLT3-ITD-negative THP-1 cells because specific inhibition of FLT3 caused significant apoptosis by 51% and 78% at 24 and 96 hours of treatment, respectively. Compared with ITD negative patients with AML, Tandutinib preferentially inhibited the explosive colony growth in FLT3 ITD positive patients with AML, but did not affect the colony formation of normal human progenitor cells. The addition of low nanomolar Tandutinib significantly reduced the amount of Cytarabine or Daunorubicin, which is necessary to obtain the antiproliferative effect, indicating that the combination of Tandutinib and Cytarabine/Daunorubicin greatly enhances the synergistic effect. |
| In vivo study | Tandutinib administered orally at a dose of 60 mg/kg twice daily significantly increased the lifespan of mice carrying Ba/F3 cells expressing the W51 FLT3-ITD mutant, while acting on a mouse bone marrow transplantation model, significantly reduced mortality. Tandutinib at a dose of 180 mg/kg twice a day is slightly toxic to normal hematopoietic function, and Tandutinib is effective in the treatment of FLT3 ITD-positive leukemia in mice. |
Tandutinib (MLN518) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.777 ml | 8.885 ml | 17.771 ml |
| 5 mM | 0.355 ml | 1.777 ml | 3.554 ml |
| 10 mM | 0.178 ml | 0.889 ml | 1.777 ml |
| 5 mM | 0.036 ml | 0.178 ml | 0.355 ml |
Last Update：2024-01-02 23:10:35
Tandutinib (MLN518) - Reference Information
| Product description | Tandotinib is a new type of oral small molecule multi-target receptor tyrosine kinase developed by Millennium Pharmaceutical Company (Millennium) Inhibitor, a synthetic piperquinazoline compound, mainly for the treatment of acute myeloid leukemia, multiple myeloma and myelodysplastic syndrome. It has inhibitory effects on receptor tyrosine kinase, including FMS-like tyrosine kinase -3 (FLT-3), PDGFR and stem cell factor receptor (c-KitR). Tandotinib inhibits phosphorylation of FLT-3. In a phase I clinical trial, 40 patients with AML and myelodysplastic syndrome (MDS) were given oral tandotinib. The results showed that the maximum tolerated dose (MTD) was 525mg(bid) and showed certain activity. At present, tandotinib has entered phase II clinical study. List of related drugs: Gefitinib mesylate imatinanirapatinib maleate sunitininirotinib pazopazopanibosutininib cecatinib axitinib maritinib sunitinib malate |
| molecular structure | 1. molar refractive index: 160.96 2. molar volume (m3/mol):463.8 3. isotonic specific volume (90.2K):1261.7 4. surface tension (dyne/cm):54.7 5. polarizability (10-24cm3):63.81 |
| application | anti-cancer bulk drug, a new immunomodulatory drug, is mainly used for the treatment of multiple myeloma and myelodysplastic syndrome; for the synthesis of organic raw materials or drug intermediates; synthetic research in scientific research units; scientific research reagents are widely used in molecular biology, pharmacology and other scientific research aspects. |
| Effect | Tandotinib is a new type of oral small molecule multi-target receptor tyrosine kinase developed by Millennium Pharmaceutical Company (Millennium) Inhibitor, a synthetic piperquinazoline compound, mainly for the treatment of acute myeloid leukemia, multiple myeloma and myelodysplastic syndrome. It has inhibitory effects on receptor tyrosine kinase, including FMS-like tyrosine kinase -3 (FLT-3), PDGFR and stem cell factor receptor (c-KitR). |
| biological activity | Tandutinib (MLN518, CT53518, NSC726292) is an effective FLT3 antagonist with IC50 of 0.22 μM, and also inhibits PDGFR and c-Kit. the effect on FLT3 is 15 to 20 times stronger than that of CSF-1R, and more than 100 times stronger than that of FGFR, EGFR and KDR. Phase 2. |
| Target | Value |
| c-Kit | 0.17 μM |
| PDGFRβ | 0.20 μM |
| FLT3 () | 0.22 μM |
| CSF-1R | 3.43 μM |
Last Update：2024-04-10 22:29:15
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Spot supply
Product Name: MLN518; CT53518 Visit Supplier Webpage Request for quotationCAS: 387867-13-2
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: Tandutinib Visit Supplier Webpage Request for quotationCAS: 387867-13-2
Tel: +86 0571-86722205
Email: sales@chinaskyrun.com
Mobile: +8618958170122
QQ: 2531159185
Wechat: chinaskyrun
Spot supply
Product Name: Tandutinib (MLN518) Visit Supplier Webpage Request for quotationCAS: 387867-13-2
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: Tandutinib (MLN518) Visit Supplier Webpage Request for quotationCAS: 387867-13-2
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Spot supply
Product Name: Tandutinib (MLN518) Visit Supplier Webpage Request for quotationCAS: 387867-13-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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