ENMD-2076
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 | $960 | Check With Us |
| 500mg | $1450 | Check With Us |
| 1g | $2175 | Check With Us |
: Cat #: V0363 CAS #: 934353-76-1 (free base) Purity ≥ 98%
Description: ENMD-2076 (ENMD2076) is a novel,potent and orally bioactive inhibitor of multikinase including Aurora A and Flt3 with potential antitumor activity.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 375.47 |
|---|---|
| Molecular Formula | C21H25N7 |
| CAS No. | 934353-76-1 (free base) |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 105 mg/mL (279.6 mM)r |
| Water: 1 mg/mL (2.7 mM)r | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 0.5% CMC+0.25% Tween 80: 30 mg/mL |
| SMILES Code | CN1CCN(C2=CC(NC3=NNC(C)=C3)=NC(/C=C/C4=CC=CC=C4)=N2)CC1 |
| Synonyms | ENMD 2076; ENMD-2076; ENMD2076 |
| Protocol | In Vitro | ENMD-2076 is selective toward Aurora A versus Aurora B (IC50=350 nM). ENMD-2076 inhibits HUVEC growth with an IC50 value of 0.15 mM. Against 10 human leukemia cell lines, the IC50 values range from 0.025 to 0.53 mM. Within this panel, MV4:11 cells are the most sensitive cells by a factor of greater than 4. The lymphoma-derived U937 cell line treated with ENMD-2076 shows that the ENMD-2076 induces a dose-dependent increase in G2-M-phase arrest as well as the induction of apoptosis. ENMD-2076 inhibits cellular Flt3 ligand (FL)-induced Flt3 autophosphorylation in THP-1 cells, which have been shown to express FL-responsive wild-type Flt- 3 (18) with an IC50 value of 28 nM. ENMD-2076 inhibits stem cell factor (SCF)-induced Kit autophosphorylation in MO7e cells with an IC50 value of 40 nM. ENMD-2076 inhibits VEGFR2/KDR autophosphorylation with an IC50 value of 7 nM. |
|---|---|---|
| In Vivo | ENMD-2076 treatment results in statistically significant, dose dependent inhibition of tumor growth or tumor regression. Moreover, there is no correlation between tumor growth rate and antitumor efficacy, which would conceivably be expected for a mitotic kinase inhibitor, as fast growing (e.g., A375 melanoma) and slow-growing (e.g., HT29 colon carcinoma) tumors are similarly inhibited by ENMD-2076. ENMD-2076 is well tolerated at daily doses up to 302 mg/kg (equivalent to 200 mg/kg of the free base), with no weight loss or signs of morbidity noted in any study at this dose with the exception of the A375 model. |
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 | 2.6633 mL | 13.3166 mL | 26.6333 mL | 53.2666 mL |
| 5mM | 0.5327 mL | 2.6633 mL | 5.3267 mL | 10.6533 mL |
| 10mM | 0.2663 mL | 1.3317 mL | 2.6633 mL | 5.3267 mL |
| 20mM | 0.1332 mL | 0.6658 mL | 1.3317 mL | 2.6633 mL |
The molarity calculator equation
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Step One: Enter information below
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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
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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.