ENMD-2076 Tartrate
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 | $750 | Check With Us |
| 1g | $1050 | Check With Us |
| 5g | $2660 | Check With Us |
: Cat #: V0528 CAS #: 1291074-87-7 Purity ≥ 98%
Description: ENMD-2076 Tartrate, the tartrate salt of ENMD-981693 (MKC-1693), is a novel, potent and orally bioactive multi-kinase inhibitor with potential antineoplastic activity.
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| Molecular Weight (MW) | 525.56 |
|---|---|
| Molecular Formula | C25H31N7O6 |
| CAS No. | 1291074-87-7 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 100 mg/mL (190.3 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 30% PEG400+0.5% Tween80+5% propylene glycol: ~30 mg/mL |
| SMILES Code | CN1CCN(C2=CC(NC3=NNC(C)=C3)=NC(/C=C/C4=CC=CC=C4)=N2)CC1 |
| Synonyms | ENMD2076 tartrate; ENMD2076; ENMD 2076; ENMD-2076 |
| 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 | 1.9027 mL | 9.5137 mL | 19.0273 mL | 38.0546 mL |
| 5mM | 0.3805 mL | 1.9027 mL | 3.8055 mL | 7.6109 mL |
| 10mM | 0.1903 mL | 0.9514 mL | 1.9027 mL | 3.8055 mL |
| 20mM | 0.0951 mL | 0.4757 mL | 0.9514 mL | 1.9027 mL |
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Step Two: Enter the in vivo formulation
%DMSO
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%Tween 80
+
%ddH2O
Calculation Results:
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Method for preparing DMSO master liquid:
mg
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,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.