生物活性
Roscovitine (Seliciclib)是一种CDK抑制剂，可优先抑制多种酶靶标，包括CDK2，CDK7和CDK9。
Targets
| Target | Value |
| CDK5/p35 | IC50: 0.16μM |
| Cdc2/CyclinB | IC50: 0.65μM |
| CDK2/CyclinA | IC50: 0.7μM |
| CDK2/CyclinE | IC50: 0.7μM |
| ERK2 | IC50: 14μM |
| GST-ERK1 | IC50: 30μM |
| ERK1 | IC50: 34μM |
| CDK4/CyclinD1 | IC50: >100μM |
| CDK6/CyclinD3 | IC50: >100μM |
| PKCα | IC50: >100μM |
| PKCβ1 | IC50: >100μM |
| PKCβ2 | IC50: >100μM |
| PKCγ | IC50: 100μM |
| PKCε | IC50: >100μM |
| PKCη | IC50: >100μM |
| c-Src | IC50: 250μM |
| PKCδ | IC50: >1000μM |
| PKCζ | IC50: >1000μM |
| v-Abl | IC50: >1000μM |
化学数据
| 目录号 | A10806 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 354.5 |
| Formula | C19H26N6O |
| 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. | 186692-46-6 |
| Synonyms | CYC202, Seliciclib |
| SMILES | CC[C@H](CO)NC1=NC2=C(C(=N1)NCC3=CC=CC=C3)N=CN2C(C)C |
溶解度
| In vitro (25°C) | DMSO | 69 mg/mL (194.67 mM) |
| Water | Insoluble |
| Ethanol | 6 mg/mL (16.92 mM) |
| In vivo | 1% DMSO+10% Tween 80+20% N-N-dimethylacetamide+69% PEG 400 | 4 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 | 28.21 mL | 141.04 mL | 282.09 mL |
| 0.5 mM | 5.64 mL | 28.21 mL | 56.42 mL |
| 1 mM | 2.82 mL | 14.1 mL | 28.21 mL |
| 5 mM | 0.56 mL | 2.82 mL | 5.64 mL |
*The above data is based on the productmolecular weight 354.5 . 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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