UMI-77
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 | $1020 | Check With Us |
| 500mg | $1480 | Check With Us |
| 1g | $2220 | Check With Us |
: Cat #: V0009 CAS #: 518303-20-3 Purity ≥ 98%
Description: UMI-77 (UMI 77; UMI77) is a novel, potent and selective Mcl-1 (Myeloid cell leukemia-1) inhibitor with Ki of 490 nM.
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- Related Biological Data
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| Molecular Weight (MW) | 468.34 |
|---|---|
| Molecular Formula | C18H14BrNO5S2 |
| CAS No. | 518303-20-3 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 93 mg/mL (198.6 mM)r |
| Water: <1 mg/mL (slightly soluble or insoluble)r | |
| Ethanol: Not available | |
| Solubility In Vivo | 5% DMSO+30% PEG 300+dd H2O: 6 mg/mL |
| SMILES Code | C1=CC=C2C(=C1)C(=CC(=C2O)SCC(=O)O)NS(=O)(=O)C3=CC=C(C=C3)Br |
| Synonyms | UMI-77, UMI77, UMI 77 |
| Protocol | In Vitro | Competitive binding curve of UMI-77 against Mcl-1 is obtained by FP based binding assay using fluorescent labeled Bid BH3 peptide with an IC50 of 1.87±0.22 μM. UMI-77 potently inhibits the cell growth of BxPC-3 and Panc-1 cell lines with IC50 values of 3.4 μM and 4.4 μM respectively, and shows 3 to 5 times less potency in inhibition of the cell growth of two other tested cell lines MiaPaCa-2 (12.5 μM) and AsPC-1 (16.1 μM). The cell growth inhibition potency of UMI-77 correlates with the highest expression of Mcl-1 and Bak, and lowest expression of Bcl-xL in the sensitive cell lines, BxPC-3 and Panc-1. Capan-2 cells are showing similar sensitivity to UMI-77 (IC50 of 5.5 μM) as BxPC-3 and Panc-1, although has low Mcl-1 levels. |
|---|---|---|
| In Vivo | UMI-77 exhibits moderate metabolic stability with a half-life of 45 minutes.The maximum tolerated dose (MTD) of UMI-77 in SCID mice is determined. Administered 60 mg/kg i.v. for 5 consecutive days per week for two weeks does not cause any loss in the animal weight and there is no obvious sign of toxicity during the course of the treatment. Increasing the dose to 80 mg/kg show severe animal weight loss (>20%), therefore 60 mg/kg is used as a therapeutic dose for the in vivo efficacy studies. Daily treatment with UMI-77 for 5 consecutive days a week for two weeks results in statistically significant tumor growth inhibition by 65% and 56% in comparison with the controls in day 19 (p<0.0001) and day 22 (p<0.003) respectively. |
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 | 2.1352 mL | 10.6760 mL | 21.3520 mL | 42.7040 mL |
| 5mM | 0.4270 mL | 2.1352 mL | 4.2704 mL | 8.5408 mL |
| 10mM | 0.2135 mL | 1.0676 mL | 2.1352 mL | 4.2704 mL |
| 20mM | 0.1068 mL | 0.5338 mL | 1.0676 mL | 2.1352 mL |
The molarity calculator equation
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The dilution calculator equation
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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.