MK-4101
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 |
|---|---|---|
| 250mg | $1080 | Check With Us |
| 500mg | $1650 | Check With Us |
| 1g | $2475 | Check With Us |
: Cat #: V2914 CAS #: 935273-79-3 Purity ≥ 98%
Description: MK-4101 is a novel, potent and selective SMO inhibitor/antagonist of the Hedgehog (Hh) signaling pathway.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 493.47 |
|---|---|
| Molecular Formula | C24H24F5N5O |
| CAS No. | 935273-79-3 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 98 mg/mL (198.59 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 60 mg/mL (121.58 mM) | |
| SMILES Code | FC(C1=CC=CC=C1C2=NN=C(C34CCC(C5=NOC(C6CC(F)(F)C6)=N5)(CC4)CC3)N2C)(F)F |
| Synonyms | MK-4101; MK 4101; MK4101 |
| Protocol | In Vitro | MK-4101 inhibits Hh signaling both in a reporter gene assay in an engineered mouse cell line with an IC50 of 1.5 µM, and in human KYSE180 oesophageal cancer cells with an IC50 of 1 µM. MK-4101 displaces a fluorescently-labeled cyclopamine derivative from 293 cells expressing recombinant human SMO with an IC50 of 1.1 µM, implying that the compound binds to SMO. MK4101 also inhibits the proliferation of medulloblastoma cells derived from neonatallyirradiated Ptch1-/+ mice in vitro with an IC50 of 0.3 µM |
|---|---|---|
| In Vivo | MK-4101 (40-80 mg/kg; oral administration; for 3.5 weeks; CD1 nude female mice) treatment shows tumor growth inhibition (40 and 80 mg/kg ) and tumor regression at the highest dose (80 mg/kg). MK-4101 treatment shows a dose-dependent down-regulation of Gli1 mRNA. The maximum effect for tumor inhibition and hedgehog pathway downregulation is achieved at 80 mg/kg | |
| Animal model | 5-weeks old CD1 nude female mice with medulloblastoma/BCC cells | |
| Dosages | 40 or 80 mg/kg once a day, 80 mg/kg twice a day | |
| Administration | Oral administration; for 3.5 weeks |
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 | 2.0265 mL | 10.1323 mL | 20.2647 mL | 40.5293 mL |
| 5mM | 0.4053 mL | 2.0265 mL | 4.0529 mL | 8.1059 mL |
| 10mM | 0.2026 mL | 1.0132 mL | 2.0265 mL | 4.0529 mL |
| 20mM | 0.1013 mL | 0.5066 mL | 1.0132 mL | 2.0265 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start)
×
Volume(start)
=
Concentration(final)
×
Volume(final)
This equation is commonly abbreviated as: C1 V1 = C2 V2
Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
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.