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.