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Motesanib也称为AMG-706，是一种有效的ATP竞争性的VEGFR1/2/3抑制剂，IC50分别为2 nM/3 nM/6 nM；对Kit具有相似的抑制活性，对VEGFR选择性比PDGFR和Ret高10倍。
Targets
| Target | Value |
|---|---|
| VEGFR1 | IC50: 2nM |
| VEGFR2 | IC50: 3nM |
| VEGFR2/Flk1 | IC50: 6nM |
| VEGFR3 | IC50: 6nM |
| Kit | IC50: 8nM |
| RET | IC50: 59nM |
| PDGFR | IC50: 84nM |
| FGFR | IC50: >2.8μM |
| EGFR | IC50: >3μM |
| Src | IC50: >3μM |
| p38 | IC50: >3μM |
| In vitro (25°C) | DMSO | Warmed: 88 mg/mL (154.54 mM) | |
| Water | Warmed: 17 mg/mL (29.85 mM) | ||
| Ethanol | Insoluble | ||
| In vivo | Saline | 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. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 17.56 mL | 87.81 mL | 175.62 mL |
| 0.5 mM | 3.51 mL | 17.56 mL | 35.12 mL |
| 1 mM | 1.76 mL | 8.78 mL | 17.56 mL |
| 5 mM | 0.35 mL | 1.76 mL | 3.51 mL |
*The above data is based on the productmolecular weight 569.4 . 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.
| 目录号 | A10608 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 569.4 |
| Formula | C22H23N5O.2H3PO4 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 857876-30-3 |
| Synonyms | AMG-706 |
| SMILES | CC1(CNC2=C1C=CC(=C2)NC(=O)C3=C(N=CC=C3)NCC4=CC=NC=C4)C.OP(=O)(O)O.OP(=O)(O)O |
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