生物活性
Tandutinib (MLN518)是一种有效的FLT3抑制剂，c-KIT和PDGF受体酪氨酸激酶的自磷酸化，从而抑制细胞增殖并诱导细胞凋亡。
Targets
| Target | Value |
| c-Kit | IC50: 0.17μM |
| PDGFRβ | IC50: 0.20μM |
| FLT3 | IC50: 0.22μM |
| CSF-1R | IC50: 3.43μM |
| Src | IC50: 30μM |
| Abl | IC50: >30μM |
| PKC | IC50: >30μM |
| PKA | IC50: >30μM |
| MEK1 | IC50: >30μM |
| MKK4 | IC50: >30μM |
| MKK6 | IC50: >30μM |
| ERK2 | IC50: >30μM |
| p38 | IC50: >30μM |
| KDR | IC50: >30μM |
| EGFR | IC50: >30μM |
| FGFR | IC50: >30μM |
| Insulin Receptor | IC50: >30μM |
化学数据
| 目录号 | A10887 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 562.7 |
| Formula | C31H42N6O4 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 387867-13-2 |
| Synonyms | MLN-518, CT53518 |
| SMILES | CC(C)OC1=CC=C(C=C1)NC(=O)N2CCN(CC2)C3=NC=NC4=CC(=C(C=C43)OC)OCCCN5CCCCC5 |
溶解度
| In vitro (25°C) | DMSO | 5 mg/mL (8.88 mM) |
| Water | Insoluble |
| Ethanol | 6 mg/mL (10.66 mM) |
| In vivo | 0.5% methylcellulose | 28 mg/mL |
*<1 mg/ml means slightly soluble or insoluble.
*Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 17.77 mL | 88.86 mL | 177.71 mL |
| 0.5 mM | 3.55 mL | 17.77 mL | 35.54 mL |
| 1 mM | 1.78 mL | 8.89 mL | 17.77 mL |
| 5 mM | 0.36 mL | 1.78 mL | 3.55 mL |
*The above data is based on the productmolecular weight 562.7 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
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