BDP5290
Based on 1 Customer Validation
BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 98.90%
- CAS No.: 1817698-21-7
- 화학식: C17H18ClN7O
- 분자량:371.82
-
보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
제품 설명
IC50 & Target
[1]|
ROCK1 5 nM (IC50) |
ROCK2 50 nM (IC50) |
MRCKα 10 nM (IC50) |
MRCKβ 100 nM (IC50) |
In Vitro
The Ki of BDP5290 for MRCKα is 10 nM, which is slightly more than the Ki of 4 nM for MRCKβ. 3 μM BDP5290 completely inhibits myosin II light chain (MLC) phosphorylation induced by MRCKβ, but not by ROCK1 or ROCK2. At higher concentrations, BDP5290 reduces MLC phosphorylation (pMLC) to undetectable levels. BDP5290 reduces MDA-MB-231 invasion at all tested concentrations starting from 0.1 μM, with virtually complete inhibition at 10 μM. After 24 hours in the presence of BDP5290 cell viability is slightly reduced with an EC50 >10 μM. Wound closure is inhibited by >60% at 1 μM BDP5290, a concentration that has no effect on cell viability[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1817698-21-7
-
Appearance Solid
-
분자량 371.82
-
화학식 C17H18ClN7O
-
Color White to off-white
-
SMILES
ClC(C(C(NC1=CNN=C1C2=NC=CC=C2)=O)=N3)=CN3C4CCNCC4
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
In Vitro:
DMSO : 12.5 mg/mL (33.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
-
Data Sheet (279 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
References
[1]. Gandalovi?ová A, et al. Migrastatics-Anti-metastatic and Anti-invasion Drugs: Promises and Challenges. Trends Cancer. 2017 Jun;3(6):391-406. [Content Brief]
[2]. Unbekandt M, et al. A novel small-molecule MRCK inhibitor blocks cancer cell invasion. Cell Commun Signal. 2014 Oct 5;12:54. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6895 mL | 13.4474 mL | 26.8947 mL | 67.2368 mL |
| 5 mM | 0.5379 mL | 2.6895 mL | 5.3789 mL | 13.4474 mL | |
| 10 mM | 0.2689 mL | 1.3447 mL | 2.6895 mL | 6.7237 mL | |
| 15 mM | 0.1793 mL | 0.8965 mL | 1.7930 mL | 4.4825 mL | |
| 20 mM | 0.1345 mL | 0.6724 mL | 1.3447 mL | 3.3618 mL | |
| 25 mM | 0.1076 mL | 0.5379 mL | 1.0758 mL | 2.6895 mL | |
| 30 mM | 0.0896 mL | 0.4482 mL | 0.8965 mL | 2.2412 mL |