DCLK1-IN-1
目录号 : GC39486
DCLK1-IN-1 is a selective, in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1) domain that binds to DCLK1 and DCLK2 with IC50 of 9.5 nM and 31 nM, respectively. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases with IC50 of 57.2 nM and 103 nM in kinase assay, respectively.
Cas No.:2222635-15-4
Sample solution is provided at 25 µL, 10mM.
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DCLK1-IN-1 is a selective, in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1) domain that binds to DCLK1 and DCLK2 with IC50 of 9.5 nM and 31 nM, respectively. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases with IC50 of 57.2 nM and 103 nM in kinase assay, respectively.
DCLK1-IN-1 displays pronounced on-target DCLK1 activity in vitro. DCLK1-IN-1 potently binds DCLK1 in HCT116 cells (IC50 = 279 nM). DCLK1-IN-1 significantly inhibits DCLK1, and weakly inhibits ERK5, in PATU-8988T cell lysates and live cells.[1]
DCLK1-IN-1 has a favorable pharmacokinetic profile in mice, with a half-life of 2.09 h, an area under the curve of 5,506 h ng?1 ml?1 and 81% oral bioavailability. DCLK1-IN-1 is well-tolerated at doses up to 100 mg kg?1 with no adverse effects and no loss of body weight observed in mice. DCLK1-IN-1 is a selective inhibitor of DCLK1, suitable for use as a chemical probe when used together with control compound DCLK1-NEG.[1]
[1] Fleur M Ferguson, et al. Nat Chem Biol. 2020 Jun;16(6):635-643.
| Cas No. | 2222635-15-4 | SDF | |
| Canonical SMILES | O=C1N(CC(F)(F)F)C2=CN=C(NC3=CC=C(N4CCN(C)CC4)C=C3OC)N=C2N(C)C5=CC=CC=C15 | ||
| 分子式 | C26H28F3N7O2 | 分子量 | 527.54 |
| 溶解度 | DMSO: 35.71 mg/mL (67.69 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8956 mL | 9.478 mL | 18.9559 mL |
| 5 mM | 0.3791 mL | 1.8956 mL | 3.7912 mL |
| 10 mM | 0.1896 mL | 0.9478 mL | 1.8956 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet