Synonym
MRT67307; MRT-67307; MRT 67307; MRT67307 HCl. MRT67307 hydrochloride
IUPAC/Chemical Name
N-(3-((2-cyclopropyl-5-((2-methyl-1,2,3,4-tetrahydroisoquinolin-6-yl)amino)phenyl)amino)propyl)cyclobutanecarboxamide dihydrochloride
InChi Key
AVTUJIVDDXSHKB-UHFFFAOYSA-N
InChi Code
InChI=1S/C27H36N4O.2ClH/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);2*1H
SMILES Code
O=C(C1CCC1)NCCCNC2=CC(NC3=CC4=C(CN(C)CC4)C=C3)=CC=C2C5CC5.[H]Cl.[H]Cl
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, not in water
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
Related CAS#
CAS#1190379-70-4 ( MRT67307HCl);
CAS#1190378-57-4 ( MRT67307 free base)
Autophagy is a cell-protective and degradative process that recycles damaged and long-lived cellular components. Cancer cells are thought to take advantage of autophagy to help them to cope with the stress of tumorigenesis; thus targeting autophagy is an attractive therapeutic approach
Biological target:
MRT67307 is a potent ULK inhibitor and SIK inhibitor.
In vitro activity:
10 μm MRT67307 was sufficient to reduce phospho-ATG13 to control levels, and in line with the in vitro IC50 values, 10-fold less MRT68921 (1 μm) resulted in a similar reduction.
Reference: J Biol Chem. 2015 May 1;290(18):11376-83. https://pubmed.ncbi.nlm.nih.gov/25833948/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
53.8 |
106.32 |
| Ethanol |
92.0 |
181.99 |
| Water |
51.4 |
101.63 |
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
505.53
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.
| 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. 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. Epub 2015 Apr 1. Erratum in: J Biol Chem. 2015 Nov 27;290(48):28726. PMID: 25833948; PMCID: PMC4416842.
In vitro protocol:
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. Epub 2015 Apr 1. Erratum in: J Biol Chem. 2015 Nov 27;290(48):28726. PMID: 25833948; PMCID: PMC4416842.
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. Epub 2015 Apr 1. Erratum in: J Biol Chem. 2015 Nov
27;290(48):28726. PubMed PMID: 25833948; PubMed Central PMCID: PMC4416842.
2: Clark K, MacKenzie KF, Petkevicius K, Kristariyanto Y, Zhang J, Choi HG,
Peggie M, Plater L, Pedrioli PG, McIver E, Gray NS, Arthur JS, Cohen P.
Phosphorylation of CRTC3 by the salt-inducible kinases controls the
interconversion of classically activated and regulatory macrophages. Proc Natl
Acad Sci U S A. 2012 Oct 16;109(42):16986-91. doi: 10.1073/pnas.1215450109. Epub
2012 Oct 2. PubMed PMID: 23033494; PubMed Central PMCID: PMC3479463.
3: Clark K, Peggie M, Plater L, Sorcek RJ, Young ER, Madwed JB, Hough J, McIver
EG, Cohen P. Novel cross-talk within the IKK family controls innate immunity.
Biochem J. 2011 Feb 15;434(1):93-104. doi: 10.1042/BJ20101701. PubMed PMID:
21138416.
