LDN-212854 |
| Catalog No.GC17035 |
LDN-212854는 ALK2(IC50: 1.3nM)를 강력하게 억제하는 BMP(Bone morphogenetic protein) 억제제입니다. LDN-212854는 또한 ALK1(IC50: 2.40nM)을 억제합니다. LDN-212854는 진행성 섬유 이형성증 및 간세포 암종(HCC)과 같은 암의 연구에 사용할 수 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1432597-26-6
Sample solution is provided at 25 µL, 10mM.
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LDN-212854 is a selective inhibitor of bone morphogenetic protein (BMP) signaling with IC50 value of 1.2nM [1].
In the kinase assay, LDN-212854 shows inhibitory activities against caALK2 and caALK5 with IC50 values of 16nM and 2μM, respectively. It demonstrates that LDN-212854 is selective against BMP over TGF-β signaling. Besides that, the inhibition of caALK2 caused by LDN-212854 is 6- and 10-fold more potent than that of caALK1 and caALK3, respectively. In C2C12 cells transfected with BMP receptors, LDN-212854 also exerts preferential inhibition against caALK2. Furthermore, in a transgenic ALK2Q207D model of heterotopic ossification, treatment of LDN-212854 prevents the formation of heterotopic bone and preserves limb range of motion [1].
References:
[1] Mohedas A H, Xing X, Armstrong K A, et al. Development of an ALK2-biased BMP type I receptor kinase inhibitor. ACS chemical biology, 2013, 8(6): 1291-1302.
| Cas No. | 1432597-26-6 | SDF | |
| Canonical SMILES | C1CN(CCN1)C2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=C6C=CC=NC6=CC=C5)N=C3 | ||
| Formula | C25H22N6 | M.Wt | 406.48 |
| Solubility | ≥ 20.3mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4601 mL | 12.3007 mL | 24.6015 mL |
| 5 mM | 492 μL | 2.4601 mL | 4.9203 mL |
| 10 mM | 246 μL | 1.2301 mL | 2.4601 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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