EPZ004777
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 | $1320 | Check With Us |
| 500mg | $1950 | Check With Us |
| 1g | $2925 | Check With Us |
: Cat #: V0401 CAS #: 1338466-77-5 (free) Purity ≥ 98%
Description: EPZ004777 (EPZ-004777) is a potent and selective inhibitor of DOT1 Like Histone Lysine Methyltransferase (DOT1L) inhibitor with antineoplastic activity.
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| Molecular Weight (MW) | 539.67 |
|---|---|
| Molecular Formula | C28H41N7O4 |
| CAS No. | 1338466-77-5 (free) |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 100 mg/mL (185.3 mM)r |
| Water:<1 mg/mLr | |
| Ethanol: 100 mg/mL (185.3 mM) | |
| SMILES Code | O=C(NC1=CC=C(C(C)(C)C)C=C1)NCCCN(C[C@H]2O[C@@H](N3C=CC4=C(N)N=CN=C43)[C@H](O)[C@@H]2O)C(C)C |
| Synonyms | EPZ 004777; EPZ-004777; EPZ004777 |
| Protocol | In Vitro | EPZ004777 demonstrates potent, concentration-dependent inhibition of DOT1L enzyme activity with an IC50 of 400±100 pM. EPZ004777 displays remarkable selectivity for inhibition of DOT1L over other HMTs(PRMT5, 521±137 nM; others, >50 μM). The effect of extended EPZ004777 treatment is remarkably specific for the MLL-rearranged cell lines. The number of viable MV4-11 and MOLM-13 cells is dramatically reduced by EPZ004777, whereas the growth of Jurkat cells is unaffected. A small population of MV4-11 cells remain viable in the presence of EPZ004777, but their number remain constant when growth curves are tracked over longer periods indicating that they have ceased to divide. The proliferation of MLL-AF9-transformed cells is strongly inhibited by EPZ004777 at concentrations of 3 μM or greater. |
|---|---|---|
| In Vivo | EPZ004777 is well tolerated and no overt toxicity is observed. Complete blood count analysis after 14 days of continuous exposure to EPZ004777 revealed a statistically significant increase in the total white blood cell count, which resulted from an increase in neutrophils, monocytes, and lymphocytes. EPZ004777 (50, 100, or 150 mg/mL) administration is well tolerated, and no significant weight loss is observed. |
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 | 1.8530 mL | 9.2649 mL | 18.5298 mL | 37.0597 mL |
| 5mM | 0.3706 mL | 1.8530 mL | 3.7060 mL | 7.4119 mL |
| 10mM | 0.1853 mL | 0.9265 mL | 1.8530 mL | 3.7060 mL |
| 20mM | 0.0926 mL | 0.4632 mL | 0.9265 mL | 1.8530 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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The dilution calculator equation
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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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.