AZD-5991

Name: AZD-5991
Brand: MedChemExpress
SKU: HY-101533
Rating: 5.0 (9 reviews)

Cat. No.: HY-101533 Purity: 99.79%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

AZD-5991 is a potent and selective Mcl-1 inhibitor with an IC₅₀ of 0.7 nM in FRET assay and a K_d of 0.17 nM in surface plasmon resonance (SPR) assay.

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

AZD-5991 Chemical Structure

CAS No. : 2143061-81-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 518	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 518	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1650	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of AZD-5991:

AZD-5991 Racemate Get quote
AZD-5991 (S-enantiomer) Get quote

9 Publications Citing Use of MCE AZD-5991

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Bcl-2 Family Isoform Specific Products:

View All Isoforms

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

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

AZD-5991 is a potent and selective Mcl-1 inhibitor with an IC₅₀ of 0.7 nM in FRET assay and a K_d of 0.17 nM in surface plasmon resonance (SPR) assay^[1].

IC₅₀ & Target^[1]

Mcl-1

0.7 nM (IC₅₀)

Mcl-1

0.17 nM (Kd)

Cellular Effect

Cell Line	Type	Value	Description	References
K562	IC₅₀	29.6 μM Compound: 5; AZD5991	Antiproliferative activity against human K562 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]
MV4-11	IC₅₀	0.024 μM Compound: 5; AZD5991	Antiproliferative activity against human MV4-11 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]
NCI-H23	IC₅₀	0.19 μM Compound: 5; AZD5991	Antiproliferative activity against human NCI-H23 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H23 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]
NCI-H929	IC₅₀	0.036 μM Compound: 5; AZD5991	Antiproliferative activity against human NCI-H929 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H929 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]
SK-BR-3	IC₅₀	30 μM Compound: 5; AZD5991	Antiproliferative activity against human SK-BR-3 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human SK-BR-3 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]

In Vitro

The selectivity of AZD-5991 is evaluated against pro-survival Bcl-2 family members using FRET assays. AZD-5991 is selective for Mcl-1 (IC₅₀ 0.72?nM, K_i=200?pM) vs. Bcl-2 (IC₅₀=20?μM, K_i=6.8?μM), Bcl-xL (IC₅₀=36?μM, K_i=18?μM), Bcl-w (IC₅₀=49?μM, K_i=25?μM), and Bfl-1 (IC₅₀=24?μM, K_i=12?μM). MOLP-8, MV4-11, and NCI-H23 cells are treated with AZD5991 (EC₅₀=0.033, 0.024, 0.19?μM, respectively).AZD5991 binds directly to Mcl-1 and induces rapid apoptosis in cancer cells, most notably myeloma and acute myeloid leukemia, by activating the Bak-dependent mitochondrial apoptotic pathway. AZD5991 reduces the levels of Mcl-1 protein in AZD5991-sensitive but not in AZD5991-resistant MM cell lines further supporting the notion that activation of caspases by AZD5991 reduces Mcl-1 protein levels in AZD5991-sensitive cell lines^[1].

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

In Vivo

A single intravenous (i.v.) dose of AZD5991 leads to a dose-dependent antitumor effect ranging from tumor growth inhibition (TGI) to tumor regression (TR). Ten days after treatment, AZD5991 shows 52% and 93% TGI (p<0.0001) at 10 and 30?mg/kg, respectively. At the same time point, AZD5991 at 60?mg/kg leads to 99% TR with no detectable tumors in 6 out of 7 mice, while complete TR is seen in 7 out of 7 mice in the 100?mg/kg dose group. AZD5991 also shows a dose-dependent duration of response with tumors in the 100?mg/kg group growing back later than those in the 60?mg/kg group. The magnitude of in vivo tumor efficacy is correlated with activation of caspase-3 in the tumor and concentration of AZD5991 in plasma. Treatment with AZD5991 was well tolerated at all dose levels with no significant body weight loss. A single dose of AZD5991 36 days after the first dose causes tumor regression in 4 out of 4 mice. In mice dosed with AZD5991 at 100?mg/kg on day 0 and day 1, tumors grow back later than those dosed with a single dose of AZD5991 at the same dose level^[1].

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

Clinical Trial

Molecular Weight

672.26

Formula

C₃₅H₃₄ClN₅O₃S₂

CAS No.

2143061-81-6

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C1=C(CCCOC2=C(C=CC=C3)C3=CC4=C2)C5=C(N1C)C(C6=C(C)N(C)N=C6CSCC7=NN(C)C(CS4)=C7)=C(Cl)C=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (371.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.4875 mL	7.4376 mL	14.8752 mL
5 mM	0.2975 mL	1.4875 mL	2.9750 mL
10 mM	0.1488 mL	0.7438 mL	1.4875 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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: ≥ 2.08 mg/mL (3.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (3.09 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 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 (20.8 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.
Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (3.09 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 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 (20.8 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.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 6

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 99.79%

Select Batch:

Data Sheet (287 KB) SDS (393 KB)

COA (265 KB) LCMS (91 KB)

Handling Instructions (2659 KB)

References

[1]. Tron AE, et al. Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia. Nat Commun. 2018 Dec 17;9(1):5341. [Content Brief]

Animal Administration
^[1]

Mice and Rats^[1]
In mice, drugs (e.g., AZD5991; 10-100 mg/kg) are dosed intravenously in a volume of 5 mL/kg except for Venetoclax that is dosed orally in a volume of 10 mL/kg. One million MV4-11, five million MOLP-8, ten million NCI-H929 or five million OCI-AML3 cells are injected subcutaneously in the right flank of mice in a volume of 0.1 mL. In rats, AZD5991 (10-100 mg/kg) is dosed intravenously in a volume of 10 mL/kg. Ten million MV4-11 cells are injected subcutaneously in the right flank of rats in a volume of 0.1 mL. Tumor volumes (measured by caliper), animal body weight, and tumor condition are recorded twice weekly for the duration of the study. The tumor volume is calculated^[1].

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

References

[1]. Tron AE, et al. Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia. Nat Commun. 2018 Dec 17;9(1):5341. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.4875 mL	7.4376 mL	14.8752 mL	37.1880 mL
	5 mM	0.2975 mL	1.4875 mL	2.9750 mL	7.4376 mL
	10 mM	0.1488 mL	0.7438 mL	1.4875 mL	3.7188 mL
	15 mM	0.0992 mL	0.4958 mL	0.9917 mL	2.4792 mL
	20 mM	0.0744 mL	0.3719 mL	0.7438 mL	1.8594 mL
	25 mM	0.0595 mL	0.2975 mL	0.5950 mL	1.4875 mL
	30 mM	0.0496 mL	0.2479 mL	0.4958 mL	1.2396 mL
	40 mM	0.0372 mL	0.1859 mL	0.3719 mL	0.9297 mL
	50 mM	0.0298 mL	0.1488 mL	0.2975 mL	0.7438 mL
	60 mM	0.0248 mL	0.1240 mL	0.2479 mL	0.6198 mL
	80 mM	0.0186 mL	0.0930 mL	0.1859 mL	0.4648 mL
	100 mM	0.0149 mL	0.0744 mL	0.1488 mL	0.3719 mL

AZD-5991 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:

AZD-59912143061-81-6AZD5991AZD 5991Bcl-2 FamilyInhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
Product Name			Salutation
Applicant Name *			Email Address *
Phone Number *			Organization Name *
Department *			Requested quantity *
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

AZD-5991

Customer Review

Other Forms of AZD-5991:

AZD-5991 Related Antibodies

9 Publications Citing Use of MCE AZD-5991

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

AZD-5991 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

AZD-5991 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report