MRT68921 dihydrochloride

Name: MRT68921 dihydrochloride
Brand: MedChemExpress
SKU: HY-100006A
Rating: 5.0 (22 reviews)

Cat. No.: HY-100006A Purity: 99.67%: Data Sheet
COA

SDS
Handling Instructions
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MRT68921 dihydrochloride is a potent NUAK1/ULK1 dual inhibitor. MRT68921 dihydrochloride inhibits ULK1 and ULK2 with IC₅₀ values of 2.9 nM and 1.1 nM, respectively. MRT68921 dihydrochloride can block cells autophagy and kill tumor cells by breaking the balance of oxidative stress signals. MRT68921 dihydrochloride can inhibit cell proliferation and induce ROS production and apoptosis. MRT68921 dihydrochloride can be used for the research of cancer, such as breast cancer.

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

MRT68921 dihydrochloride Chemical Structure

CAS No. : 2080306-21-2

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

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Customer Review

Based on 22 publication(s) in Google Scholar

Other Forms of MRT68921 dihydrochloride:

MRT68921 In-stock
MRT68921 hydrochloride Get quote

22 Publications Citing Use of MCE MRT68921 dihydrochloride

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All ULK Isoform Specific Products:

View All Isoforms

ULK1 ULK2

View All GSK-3 Isoform Specific Products:

View All Isoforms

GSK-3 GSK-3α GSK-3β

View All Bcl-2 Family Isoform Specific Products:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[2]

ULK2

1.1 nM (IC₅₀)

ULK1

2.9 nM (IC₅₀)

GSK-3β

Bcl-2

In Vitro

MRT68921 dihydrochloride (1 μM, 1 h) reduces basal LC3 puncta and blocks basal autophagy in mouse embryonic fibroblasts (MEFs)^[1].
MRT68921 dihydrochloride (1 μM) reduces LC3-II levels in TBK1 knock-out and matched wild-type MEFs^[1].
MRT68921 dihydrochloride (24 h) exhibits cytotoxic activity in cancer cells with IC₅₀ values ranging from 1.76-8.91 μM^[2].
MRT68921 dihydrochloride (0-10 μM, 8-24 h) induces ROS production and apoptosis in NCI-H460 and MNK45 cells^[2].
MRT68921 dihydrochloride (0-5 μM, 8h) suppresses the NUAK1/MYPT1/Gsk3β andautophagy associated signaling pathway in U251 and MNK45 cells^[2].

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

Western Blot Analysis^[1]

Cell Line:	U251 and MNK45 cells
Concentration:	0, 0.5, 1, 2, 3 and 5 μM
Incubation Time:	8 h
Result:	Increased cleaved PARP1 expression. Downregulated phosphorylation of MYPT1 and Gsk3β. Increased puncta LC3.

In Vivo

MRT68921 dihydrochloride (10-40 mg/kg, s.c., daily for 7 times) inhibits tumor growth in NCI-H460 tumor mice models^[2].
MRT68921 dihydrochloride (20 mg/kg, s.c., every 2 days for 7 times) inhibits tumor growth in MNK45 tumor mice models^[2].
MRT68921 dihydrochloride (20 mg/kg, i.p., daily for 7 times) reduces the number of lung metastatic nodules in 4T1 tumor mice models^[2].

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

Animal Model:	NCI-H460 tumor mice models^[2]
Dosage:	10, 20, or 40 mg/kg
Administration:	Subcutaneously injection, daily for 7 times
Result:	Reduced tumor volume. Increased Bax levels and decreased Bcl-2 levels.

Animal Model:	MNK45 tumor mice models^[2]
Dosage:	20 mg/kg
Administration:	Subcutaneously injection, every 2 days for 7 times
Result:	Reduced tumor volume.

Animal Model:	4T1 tumor mice models^[2]
Dosage:	20 mg/kg
Administration:	Intraperitoneally injection, daily for 7 times
Result:	Reduced the number of lung metastatic nodules. Had no abnormal structures of the heart, kidney, liver, and spleen.

Molecular Weight

507.50

Formula

C₂₅H₃₆Cl₂N₆O

CAS No.

2080306-21-2

Appearance

Solid

Color

White to off-white

SMILES

[H]Cl.O=C(C1CCC1)NCCCNC2=NC(NC3=CC4=C(CN(C)CC4)C=C3)=NC=C2C5CC5.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 20.83 mg/mL (41.04 mM; ultrasonic and warming and heat to 60°C)

DMSO : 8.33 mg/mL (16.41 mM; ultrasonic and warming and heat to 60°C; 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	1.9704 mL	9.8522 mL	19.7044 mL
5 mM	0.3941 mL	1.9704 mL	3.9409 mL
10 mM	0.1970 mL	0.9852 mL	1.9704 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

μL

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

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.67%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (246 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Petherick KJ, et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem. 2015 May 1;290(18):11376-83. [Content Brief]

[2]. Chen Y, et al. Dual targeting of NUAK1 and ULK1 using the multitargeted inhibitor MRT68921 exerts potent antitumor activities. Cell Death Dis. 2020 Sep 1;11(8):712. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO / H₂O	1 mM	1.9704 mL	9.8522 mL	19.7044 mL	49.2611 mL
	5 mM	0.3941 mL	1.9704 mL	3.9409 mL	9.8522 mL
	10 mM	0.1970 mL	0.9852 mL	1.9704 mL	4.9261 mL
	15 mM	0.1314 mL	0.6568 mL	1.3136 mL	3.2841 mL
H₂O	20 mM	0.0985 mL	0.4926 mL	0.9852 mL	2.4631 mL
	25 mM	0.0788 mL	0.3941 mL	0.7882 mL	1.9704 mL
	30 mM	0.0657 mL	0.3284 mL	0.6568 mL	1.6420 mL
	40 mM	0.0493 mL	0.2463 mL	0.4926 mL	1.2315 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.