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MedKoo Cat#: 531223 | Name: MRT68921 free base
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

MRT68921 is an inhibitor of ULK1 and ULK2 (IC50s = 2.9 and 1.1 nM, respectively).

Chemical Structure

MRT68921 free base
MRT68921 free base
CAS#1190379-70-4 (free base)

Theoretical Analysis

MedKoo Cat#: 531223

Name: MRT68921 free base

CAS#: 1190379-70-4 (free base)

Chemical Formula: C27H36N4O

Exact Mass: 432.2889

Molecular Weight: 432.61

Elemental Analysis: C, 74.96; H, 8.39; N, 12.95; O, 3.70

Price and Availability

Size Price Availability Quantity
5mg USD 295.00 2 Weeks
10mg USD 500.00 2 Weeks
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Related CAS #
1190379-70-4 (free base) 2080306-21-2 (HCl)
Synonym
MRT68921; MRT-68921; MRT 68921; MRT68921 free base.
IUPAC/Chemical Name
Cyclobutanecarboxylic acid {3-[2-cyclopropyl-5-(2-methyl-1,2,3,4-tetrahydro-isoquinolin-6-ylamino)-phenylamino]-propyl}-amide
InChi Key
JGKCPXMSBDYENM-UHFFFAOYSA-N
InChi Code
InChI=1S/C27H36N4O/c1-31-15-12-21-16-23(9-8-22(21)18-31)30-24-10-11-25(19-6-7-19)26(17-24)28-13-3-14-29-27(32)20-4-2-5-20/h8-11,16-17,19-20,28,30H,2-7,12-15,18H2,1H3,(H,29,32)
SMILES Code
O=C(C1CCC1)NCCCNC2=CC(NC3=CC4=C(CN(C)CC4)C=C3)=CC=C2C5CC5
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Certificate of Analysis
View CoA: current batch, Lot#C9M03C26
Safety Data Sheet (SDS)
View Safety Data Sheet (SDS)
Instruction
View handling instruction
Biological target:
MRT68921 is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM.
In vitro activity:
Inhibition of ULK1 activity (by treatment with MRT68921) or its expression (by siRNA knockdown) in STAT3-KO cells inhibits autophagy and sensitizes cells to apoptosis. Reference: J Cell Mol Med. 2022 Jul;26(14):3873-3890. https://pubmed.ncbi.nlm.nih.gov/35670018/
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMF 5.0 11.56
DMF:PBS (pH 7.2) (1:5) 0.2 0.37
DMSO 3.0 6.93
Ethanol 2.0 4.62
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 432.61 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Bhattacharya S, Yin J, Yang C, Wang Y, Sims M, Pfeffer LM, Chaum E. STAT3 suppresses the AMPKα/ULK1-dependent induction of autophagy in glioblastoma cells. J Cell Mol Med. 2022 Jul;26(14):3873-3890. doi: 10.1111/jcmm.17421. Epub 2022 Jun 6. PMID: 35670018; PMCID: PMC9279602. 2. Avsec D, Jakoš Djordjevič AT, Kandušer M, Podgornik H, Škerget M, Mlinarič-Raščan I. Targeting Autophagy Triggers Apoptosis and Complements the Action of Venetoclax in Chronic Lymphocytic Leukemia Cells. Cancers (Basel). 2021 Sep 10;13(18):4557. doi: 10.3390/cancers13184557. PMID: 34572784; PMCID: PMC8466897.
In vitro protocol:
1. Bhattacharya S, Yin J, Yang C, Wang Y, Sims M, Pfeffer LM, Chaum E. STAT3 suppresses the AMPKα/ULK1-dependent induction of autophagy in glioblastoma cells. J Cell Mol Med. 2022 Jul;26(14):3873-3890. doi: 10.1111/jcmm.17421. Epub 2022 Jun 6. PMID: 35670018; PMCID: PMC9279602. 2. Avsec D, Jakoš Djordjevič AT, Kandušer M, Podgornik H, Škerget M, Mlinarič-Raščan I. Targeting Autophagy Triggers Apoptosis and Complements the Action of Venetoclax in Chronic Lymphocytic Leukemia Cells. Cancers (Basel). 2021 Sep 10;13(18):4557. doi: 10.3390/cancers13184557. PMID: 34572784; PMCID: PMC8466897.
In vivo protocol:
TBD
1: Petherick KJ, Conway OJ, Mpamhanga C, Osborne SA, Kamal A, Saxty B, Ganley IG. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem. 2015 May 1;290(18):11376-83. doi: 10.1074/jbc.C114.627778. Erratum in: J Biol Chem. 2015 Nov 27;290(48):28726. PubMed PMID: 25833948; PubMed Central PMCID: PMC4416842.