UMI-77

Name: UMI-77
Brand: MedChemExpress
SKU: HY-18628
Rating: 5.0 (2 reviews)

Cat. No.: HY-18628 Purity: 99.66%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 (IC₅₀=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.

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

UMI-77 Chemical Structure

CAS No. : 518303-20-3

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 103	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 103	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 47	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 312	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 650	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of UMI-77:

UMI-77-d₄ Get quote

2 Publications Citing Use of MCE UMI-77

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Mcl-1

0.49 μM (Ki)

Bfl-1

5.33 μM (Ki)

Bcl-W

8.19 μM (Ki)

Bcl-2

23.83 μM (Ki)

Bcl-xL

32.99 μM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	11.37 μM Compound: UMI-77	Antiproliferative activity against human HepG2 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells incubated for 72 hrs by MTT assay	[PMID: 32088497]
HL-60	IC₅₀	3.13 μM Compound: 10	Cytotoxicity against human HL60 cells assessed as intracellular ATP level after 3 days by CellTiterGlo assay Cytotoxicity against human HL60 cells assessed as intracellular ATP level after 3 days by CellTiterGlo assay	[PMID: 24749893]
Jurkat	IC₅₀	9.79 μM Compound: UMI-77	Antiproliferative activity against human Jurkat cells incubated for 72 hrs by MTT assay Antiproliferative activity against human Jurkat cells incubated for 72 hrs by MTT assay	[PMID: 32088497]
K562	IC₅₀	15.11 μM Compound: 10	Cytotoxicity against human K562 cells assessed as intracellular ATP level after 3 days by CellTiterGlo assay Cytotoxicity against human K562 cells assessed as intracellular ATP level after 3 days by CellTiterGlo assay	[PMID: 24749893]
MOLT-4	IC₅₀	3.14 μM Compound: UMI-77	Antiproliferative activity against human MOLT-4 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MOLT-4 cells incubated for 72 hrs by MTT assay	[PMID: 32088497]
MV4-11	IC₅₀	10.87 μM Compound: 10	Cytotoxicity against human MV4-11 cells assessed as intracellular ATP level after 3 days by CellTiterGlo assay Cytotoxicity against human MV4-11 cells assessed as intracellular ATP level after 3 days by CellTiterGlo assay	[PMID: 24749893]
NCI-H1299	IC₅₀	6.08 μM Compound: UMI-77	Antiproliferative activity against human NCI-H1299 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells incubated for 72 hrs by MTT assay	[PMID: 32088497]
PC-3	IC₅₀	8.43 μM Compound: UMI-77	Antiproliferative activity against human PC-3 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells incubated for 72 hrs by MTT assay	[PMID: 32088497]
RPMI-8226	IC₅₀	5.77 μM Compound: UMI-77	Antiproliferative activity against human RPMI-8226 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human RPMI-8226 cells incubated for 72 hrs by MTT assay	[PMID: 32088497]

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^[1].

MedChemExpress (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].

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

Molecular Weight

468.34

Formula

C₁₈H₁₄BrNO₅S₂

CAS No.

518303-20-3

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CSC1=CC(NS(=O)(C2=CC=C(Br)C=C2)=O)=C3C=CC=CC3=C1O

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.66%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (258 KB) HNMR (364 KB) RP-HPLC (98 KB) MS (69 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

Cell Assay ^[1]	Human PC cell lines AsPC-1, BxPC-3 and Capan-2 are cultured in RPMI 1640 medium, while Panc-1 and MiaPaCa are cultured in DMEM medium, all supplemented with 10% fetal bovine serum. The cell growth inhibition after treatment with increasing concentrations of the compounds (e.g., UMI-77; 1,10, and 100 μM) is determined by WST-8 assay^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] For BxPC-3 subcutaneous model, 10×10⁶ cells are subcutaneously injected into the flanks of 4-5 week old female severe combined immune deficient mice (ICR-SCID). Palpable tumors start to appear in 3-5 weeks. Tumors are measured twice weekly. To prevent any pain or discomfort, mice are euthanized and their tumors remove once they reach ~1800 mg burden. Tumors are then dissected into 50 mg pieces and re-transplanted into naïve ICR-SCID for serial propagation. Animals are treated with either vehicle or UMI-77 given i.v. (60 mg/kg) on day three post BxPC-3 transplantation for two weeks (5 days a week). Tumor weight is recorded throughout the treatment period. At the end of the treatment period, animals are euthanized and their tumors harvested for protein isolation and western blot analysis for apoptotic markers. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1352 mL	10.6760 mL	21.3520 mL	53.3800 mL
	5 mM	0.4270 mL	2.1352 mL	4.2704 mL	10.6760 mL
	10 mM	0.2135 mL	1.0676 mL	2.1352 mL	5.3380 mL
	15 mM	0.1423 mL	0.7117 mL	1.4235 mL	3.5587 mL
	20 mM	0.1068 mL	0.5338 mL	1.0676 mL	2.6690 mL
	25 mM	0.0854 mL	0.4270 mL	0.8541 mL	2.1352 mL
	30 mM	0.0712 mL	0.3559 mL	0.7117 mL	1.7793 mL
	40 mM	0.0534 mL	0.2669 mL	0.5338 mL	1.3345 mL
	50 mM	0.0427 mL	0.2135 mL	0.4270 mL	1.0676 mL

UMI-77 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

UMI-77518303-20-3UMI77UMI 77Bcl-2 FamilyInhibitorinhibitorinhibit

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UMI-77

Customer Review

Other Forms of UMI-77:

UMI-77 Related Antibodies

2 Publications Citing Use of MCE UMI-77

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Bcl-2 Family Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

UMI-77 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

UMI-77 Related Classifications

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Customer Review

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