生物活性
CHIR-124是一种新型有效的Chk1抑制剂（Chk1和Chk2的IC50：分别为0.32 nM和697 nM）。
Targets
| Target | Value |
| Chk1 | IC50: 0.3nM |
| FLT3 | IC50: 5.8nM |
| PDGFR | IC50: 6.6nM |
| GSK-3 | IC50: 23.3nM |
| Fyn | IC50: 98.8nM |
| PKA | IC50: 103.1nM |
| PKCγ | IC50: 110nM |
| LCK | IC50: 158.3nM |
| CDK2/CyclinA | IC50: 191.1nM |
| VEGFR1/FLT1 | IC50: 463.6nM |
| Cdc2/CyclinB | IC50: 505.7nM |
| VEGFR2/Flk1 | IC50: 577.9nM |
| PKCβ2 | IC50: 580nM |
| PKCα | IC50: 580nM |
| Chk2 | IC50: 697.4nM |
| FGFR3 | IC50: 1.29μM |
| bFGFR | IC50: 2.04μM |
| CDK4/CyclinD | IC50: 2.05μM |
| PKAβ1 | IC50: 2.25μM |
| c-Met | IC50: >3μM |
| ERK2 | IC50: 4.31μM |
| CABL | IC50: 14.88μM |
化学数据
| 目录号 | A11046 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 419.9 |
| Formula | C23H22ClN5O |
| 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. | 405168-58-3 |
| Synonyms | CHIR124 |
| SMILES | C1CN2CCC1[C@@H](C2)NC3=C4C=C(C=CC4=NC(=O)C3=C5NC6=CC=CC=C6N5)Cl |
溶解度
| In vitro (25°C) | DMSO | 6 mg/mL (14.29 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 1% DMSO+30% polyethylene glycol+1% Tween 80 | 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 | 23.82 mL | 119.08 mL | 238.15 mL |
| 0.5 mM | 4.76 mL | 23.82 mL | 47.63 mL |
| 1 mM | 2.38 mL | 11.91 mL | 23.82 mL |
| 5 mM | 0.48 mL | 2.38 mL | 4.76 mL |
*The above data is based on the productmolecular weight 419.9 . 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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