Sonidegib phosphate (NVP-LDE-225, Erismodegib, Odomzo)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 500mg | $650 | In Stock |
| 1g | $999 | In Stock |
| 5g | $2990 | In Stock |
: Cat #: V0099 CAS #: 1218778-77-8 Purity ≥ 98%
Description: Sonidegib phosphate or Sonidegib diphosphate, the diphosphate salt of sonidegib (also known as NVP-LDE225, Erismodegib, Sonidegib; trade name of Odomzo) is a potent and orally bioavailable small-molecule antagonist of the Smoothened (Smo) with potential anticancer activity.
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| Molecular Weight (MW) | 681.49 |
|---|---|
| Molecular Formula | C26H32F3N3O11P2 |
| CAS No. | 1218778-77-8 |
| Storage | -20℃ for 3 years in powder formrr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: >100 mg/mLrr |
| Water: N/Arr | |
| Ethanol: N/A | |
| Solubility In Vivo | 0.2% Tween-80 and 0.5% methyl cellulose |
| Synonyms | Sonidegib phosphate; Sonidegib diphosphate; LDE 225 phosphate; LDE 225 diphosphate;LDE-225 phosphate; LDE225 phosphate; LDE-225 diphosphate; LDE225 diphosphate; NVP-LDE225 diphosphate; NVP LDE-225 diphosphate; NVP-LDE225 phosphate; NVP LDE-225 phosphate; NVP LDE225 phosphate; Erismodegib phosphate; Erismodegib diphosphate; trade name of Odomzo |
| Protocol | In Vitro | The IC50 values for Sonidegib (NVP-LDE225) for the major human CYP450 drug metabolizing enzymes is greater than 10 μM[1]. Sonidegib (LDE225), a small molecule, clinically investigated SMO inhibitor, used alone and in combination with Nilotinib, inhibits the Hh pathway in CD34+ chronic phase (CP)-chronic myeloid leukaemia (CML) cells, reducing the number and self-renewal capacity of CML leukaemia stem cell (LSC). Sonidegib interacts directly with SMO, in a similar fashion to cyclopamine, to reduce expression of downstream Hh signaling targets. Primary CD34+ CP-CML cells are cultured in serum free media (SFM)±Sonidegib for 6, 24 and 72 hours (h). At 72 h, while there is variability between the biological samples, GLI1 is significantly downregulated following exposure to Sonidegib (10 nM; 0.78-fold and 100 nM; 0.73-fold, respectively (p<0.01) |
|---|---|---|
| In Vivo | Sonidegib (NVP-LDE225) is a weak base with a measured pKa of 4.2 and exhibits relatively poor aqueous solubility. In the subcutaneous Ptch+/-p53-/- medulloblastoma allograft mouse model, Sonidegib demonstrates dose-related antitumor activity after 10 days of oral administration of a suspension of the diphosphate salt. At a dose of 5 mg/kg/day qd, Sonidegib significantly inhibits tumor growth, corresponding to a T/C value of 33% (p<0.05 as compared to vehicle controls). When dosed at 10 and 20 mg/kg/day qd, Sonidegib affords 51 and 83% regression, respectively[1]. Bone marrow cells and spleen cells from a subset of treated mice are transplanted into secondary recipient mice. Transplantation of either bone marrow (BM) or spleen cells from mice treated with Sonidegib (LDE225)+Nilotinib results in reduced white cell count (WCC) and reduces leukaemia development in secondary recipients compared to Sonidegib or Nilotinib alone |
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 | 1.4674 mL | 7.3369 mL | 14.6737 mL | 29.3475 mL |
| 5mM | 0.2935 mL | 1.4674 mL | 2.9347 mL | 5.8695 mL |
| 10mM | 0.1467 mL | 0.7337 mL | 1.4674 mL | 2.9347 mL |
| 20mM | 0.0734 mL | 0.3668 mL | 0.7337 mL | 1.4674 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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Volume
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Molecular Weight*
The dilution calculator equation
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Volume(start)
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Volume(final)
This equation is commonly abbreviated as: C1 V1 = C2 V2
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C1
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V1
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
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 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.
- (2) Be sure to add the solvent(s) in order.