LDN-193189 4HCl
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 250mg | $850 | Check With Us |
| 500mg | $1350 | Check With Us |
| 1g | $2025 | Check With Us |
: Cat #: V1372 CAS #: 1062368-62-0 Purity ≥ 98%
Description: LDN193189 4HCl (LDN-193189; DM-3189; LDN 193189; DM 3189), the tetrahydrochloride salt of LDN193189, is a highly potent and selective inhibitor of the BMP (bone morphogenetic protein) signaling pathway with potential anticancer activity.
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| Molecular Weight (MW) | 552.33 |
|---|---|
| Molecular Formula | C₂₅H₂₆Cl₄N₆ |
| CAS No. | 1062368-62-0 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 1~20 mg/mL, vary from batch to batchr |
| Water: 50-100 mg/mLr | |
| Ethanol: <1 mg/mL | |
| SMILES Code | C1(C2=C3N=CC(C4=CC=C(N5CCNCC5)C=C4)=CN3N=C2)=CC=NC6=CC=CC=C16.Cl.Cl.Cl.Cl |
| Synonyms | DM3189 4HCl; LDN193189 4HCl; DM-3189 4HCl; LDN 193189 4HCl; DM 3189 4HCl; LDN-193189 4HCl |
| Protocol | In Vitro | DN193189 inhibits BMP4-mediated Smad1, Smad5 and Smad8 activation with greater potency than did dorsomorphin (IC50=5 nM versus 470 nM) while retaining 200-fold selectivity for BMP signaling versus TGF-β signaling (IC50 for TGF-β ≥1,000 nM). LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), and the TGF-β type I receptors ALK4, ALK5 and ALK7 (IC50≥500 nM) and increases selectivity for BMP signaling versus AMP-activated protein kinase, PDGFR and MAPK signaling pathways as compared to the parent compound. LDN-193189 blocks the transcriptional activity induced by either constitutively active ALK2R206H or ALK2Q207D mutant proteins. These findings suggest that LDN193189 might affect BMP-induced osteoblast differentiation. In fact, LDN193189 inhibits the induction of alkaline phosphatase activity in C2C12 cells by BMP4 even when administered 12 h after BMP stimulation, indicating sustained BMP signaling activity is needed for osteogenic differentiation |
|---|---|---|
| In Vivo | In the present study, the aim was to investigate the impact of the LDN-193189 compound, a potent inhibitor of the BMP type I receptor, on metastasis development in vivo. ZNF217-revLuc cells were injected into the left ventricle of nude mice (n = 16) while control mice (n = 13) were inoculated with control pcDNA6-revLuc cells. Mice from each group were treated or not with LDN-193189 for 35 days. We found that systemic LDN-193189 treatment of mice significantly enhanced metastasis development, by increasing both the number and the size of metastases. In pcDNA6-revLuc-injected mice, LDN-193189 also affected the kinetics of metastasis emergence. Altogether, these data suggest that in vivo, LDN-193189 might affect the interaction between breast cancer cells and the bone environment, favoring the emergence and development of multiple metastases. Hence, our report highlights the importance of the choice of drugs and therapeutic strategies used in the management of bone metastases. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.8105 mL | 9.0526 mL | 18.1051 mL | 36.2102 mL |
| 5mM | 0.3621 mL | 1.8105 mL | 3.6210 mL | 7.2420 mL |
| 10mM | 0.1811 mL | 0.9053 mL | 1.8105 mL | 3.6210 mL |
| 20mM | 0.0905 mL | 0.4526 mL | 0.9053 mL | 1.8105 mL |
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Step Two: Enter the in vivo formulation
%DMSO
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%ddH2O
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Method for preparing DMSO master liquid:
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,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 add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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