LSZ102
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 |
|---|---|---|
| 100mg | $1750 | Check With Us |
| 250mg | $3300 | Check With Us |
| 500mg | $4950 | Check With Us |
: Cat #: V3805 CAS #: 2135600-76-7 Purity ≥ 98%
Description: LSZ-102 is a potent, orally bioactive and selective ERα antagonist and SERD (estrogen receptor degrader) with an IC50 of 0.2 nM has the potential for the treatment of Estrogen Receptor Positive Breast Cancer.
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- Physicochemical and Storage Information
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| Molecular Weight (MW) | 470.46 |
|---|---|
| Molecular Formula | C25H17F3O4S |
| CAS No. | 2135600-76-7 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 10 mMr |
| Water: N/Ar | |
| Ethanol: N/A | |
| SMILES Code | O=C(O)/C=C/C1=CC=C(OC2=C(C3=CC=C(F)C=C3C(F)(F)C)SC4=CC(O)=CC=C42)C=C1 |
| Synonyms | SERD LSZ102; LSZ102; LSZ-102; LSZ 102; SERD LSZ-102; SERD LSZ 102; |
| Protocol | In Vitro | LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC50 of 0.2 nM and currently in Phase I/Ib trials for the treatment of ERα positive breast cancer. LSZ-102 induces significant degradation of ERα after 24 h, when given as a 10 μM solution to MCF-7 cells. Robust inhibition of cell proliferation in MCF-7 cells is observed upon incubation with LSZ-102 with a half inhibitory concentration of 1.7 nM. Results demonstrate that LSZ-102 effectively inhibits the estrogen-induced activation of the ERE-luciferase reporter using charcoal-stripped serum treated with E2 with IC50 of 0.3 nM. |
|---|---|---|
| In Vivo | Treatment of the mice with LSZ-102 once daily at 20 mg/kg results in significant tumor growth inhibition as compare to the control group treated with vehicle alone, resulting in tumor stasis (mean change in tumor volume of LSZ-102 vs control=%ΔT/ΔC of 2.4% on day 48, p<0.05). Dosing of 3 mg/kg solution of LSZ-102 in male Sprague-Dawley rats results in 33% bioavailability and a dose-normalized exposure of 620 nM•h. |
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 | 2.1256 mL | 10.6279 mL | 21.2558 mL | 42.5116 mL |
| 5mM | 0.4251 mL | 2.1256 mL | 4.2512 mL | 8.5023 mL |
| 10mM | 0.2126 mL | 1.0628 mL | 2.1256 mL | 4.2512 mL |
| 20mM | 0.1063 mL | 0.5314 mL | 1.0628 mL | 2.1256 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start)
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Volume(start)
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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V1
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C2
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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.