[CAS NO. 518303-20-3] UMI-77

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PRODUCTS SPECIFICATIONS [518303-20-3]

Catalog

HY-18628

Brand

MCE

CAS

518303-20-3

DESCRIPTION [518303-20-3]

Overview

MDL	MFCD03471890
Molecular Weight	468.34
Molecular Formula	C18H14BrNO5S2
SMILES	O=C(O)CSC1=CC(NS(=O)(C2=CC=C(Br)C=C2)=O)=C3C=CC=CC3=C1O

For research use only. We do not sell to patients.

1 Publications Citing Use of MCE

[1]Cancer Cell Int. 2022 Oct 7;22(1):304.

Summary

UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 ( IC ₅₀ =0.31 μM). UMI-77 binds to the BH3 binding groove of Mcl-1 with K _i of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.

IC50 & Target

IC50: 0.31±0.11 μM (Mcl-1), 10.2±2.24 μM (Bcl-2), 36.09±13.80 μM (Bcl-xL) ^[1]
Ki: 0.49±0.06 μM (Mcl-1), 5.33±1.0 μM (A1/Bfl-1), 8.19±1.91 μM (Bcl-w), 23.83±1.81 μM (Bcl-2), 32.99±4.33 μM (Bcl-xL) ^[1]

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 IC ₅₀ of 1.87±0.22 μM. UMI-77 potently inhibits the cell growth of BxPC-3 and Panc-1 cell lines with IC ₅₀ 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 (IC ₅₀ of 5.5 μM) as BxPC-3 and Panc-1, although has low Mcl-1 levels ^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 ^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 28 mg/mL ( 59.79 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1352 mL	10.6760 mL	21.3520 mL
5 mM	0.4270 mL	2.1352 mL	4.2704 mL
10 mM	0.2135 mL	1.0676 mL	2.1352 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (5.34 mM); Suspended solution; Need ultrasonic

* All of the co-solvents are available by MCE.

References

[1] Abulwerdi F, et al. A novel small-molecule inhibitor of mcl-1 blocks pancreatic cancer growth in vitro and in vivo. Mol Cancer Ther. 2014 Mar;13(3):565-575.