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MX69 - 98%, high purity , CAS No.1005264-47-0

COA COA
    Grade & Purity:
  • ≥98%
In stock
Item Number
M414002
Grouped product items
SKU Size
Availability
 Price Qty
M414002-5mg
5mg
3
$88.90
M414002-10mg
10mg
2
$147.90
M414002-25mg
25mg
2
$286.90
M414002-50mg
50mg
2
$464.90
M414002-100mg
100mg
2
$741.90
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Mdm2 Inhibitors

View related series
Amino Acid/Protein Metabolism (1836) Apoptosis (4276) E1/E2/E3 Enzyme (112) IAP (40) Intrinsic Pathway (690) MDM-2/p53 (109) Metabolic Enzyme/Protease (4860)

Basic Description

Synonyms AC-35792 | STL199512 | MX69 | MX-69 | BS-14153 | BCP19296 | EX-A2460 | C71033 | HY-100892 | 1005264-47-0 | s8403 | 4-(8-(N-(3,4-dimethylphenyl)sulfamoyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-4-yl)benzoic acid | SCHEMBL22092443 | AKOS025270161 | 4
Specifications & Purity ≥98%
Biochemical and Physiological Mechanisms MX69 is a MDM2/XIAP inhibitor that binds to MDM2 RING protein with binding Kd values of 2.34 μM. It is used for cancer treatment.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Product Description

Information

MX69 MX69 is a MDM2/XIAP inhibitor that binds to MDM2 RING protein with binding Kd values of 2.34 μM. It is used for cancer treatment.


Targets

Mdm2 (Cell-free assay) 2.34 μM(Kd)


In vitro

MX69 inhibits expression of both MDM2 and XIAP in a time- and dose-dependent manner. MX69 induces ubiquitination of endogenous MDM2 in cancer cells. Downregulation of MDM2 by MX69 is through induction of MDM2 self-ubiquitination and degradation. Half-life of MDM2 in control-treated EU-1 cells is greater than 90 min, whereas MX69 treatment decreases the MDM2 half-life to <30 min. In SK-N-SH cells with stably transfected either wild-type (WT)-MDM2 or mutant MDM2-C464A, Treatment with MX69 significantly inhibits expression and increased the turnover of WT-MDM2 but not MDM2-C464A. MX69 significantly enhances the p53 half-life in WT-MDM2 but not mutant MDM2-C464A-transfected SK-N-SH cells. p53 is stabilized and accumulates in MX69-treated cells. MX69-mediated inhibition of XIAP is MDM2 dependent. Treatment of MX69 activates caspases 3, 7, and 9 as well as the cleavage of the death substrate PARP. MX69 also exhibits a significant cytotoxic effect on both ALL and NB lines(cancer cell lines), particularly those lines with MDM2 overexpression and a WTp53 phenotype. MX69-induced cell death is indeed due to apoptosis. MX69-induced cell apoptosis and death are dependent on MDM2, p53, and XIAP expression. MX69 shows minimal inhibitory effect on normal human bone marrow in vitro.


In vivo

MX69 has significant apoptotic and anti-proliferative effects on MDM2-expressing cancer cells in vivo. MX69 is well tolerated in animals due to the fact that normal cells/tissues express little or no MDM2. No evidence of toxicity after treatment with MX69 at the 100 mg/kg dose. MDM2-specific agent MX69 should not activate either on-target (e.g., p53 induction) or off-target signaling pathways in normal cells. Thus, specific MDM2 inhibitors such as MX69 may be excellent candidates for targeted therapy of refractory cancers expressing high levels of MDM2.


Cell Research(from reference)

Cell lines：six ALL cell lines (EU-1, EU-3, EU-6, EU-8, SUP-B13, and UOC-B1) and six NB cell lines (NB-1691, NB-1643, SH-EP1, IMR-32, SK-NSH, and LA1-55N) 

Concentrations：0-10 μM 

Incubation Time：24 h 

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Quinolines and derivatives
Subclass Phenylquinolines
Intermediate Tree Nodes Not available
Direct Parent Phenylquinolines
Alternative Parents Hydroquinolines  Sulfanilides  Benzoic acids  o-Xylenes  Benzoyl derivatives  Aralkylamines  Secondary alkylarylamines  Organosulfonamides  Aminosulfonyl compounds  Amino acids  Monocarboxylic acids and derivatives  Carboxylic acids  Azacyclic compounds  Organopnictogen compounds  Organooxygen compounds  Organic oxides  Hydrocarbon derivatives  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Phenylquinoline - Sulfanilide - Tetrahydroquinoline - Benzoic acid or derivatives - Benzoic acid - O-xylene - Xylene - Benzoyl - Secondary aliphatic/aromatic amine - Aralkylamine - Benzenoid - Organosulfonic acid amide - Monocyclic benzene moiety - Aminosulfonyl compound - Sulfonyl - Organosulfonic acid or derivatives - Organic sulfonic acid or derivatives - Amino acid or derivatives - Amino acid - Carboxylic acid derivative - Carboxylic acid - Azacycle - Monocarboxylic acid or derivatives - Secondary amine - Organic nitrogen compound - Amine - Hydrocarbon derivative - Organic oxide - Organic oxygen compound - Organonitrogen compound - Organooxygen compound - Organosulfur compound - Organopnictogen compound - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as phenylquinolines. These are heterocyclic compounds containing a quinoline moiety substituted with a phenyl group.
External Descriptors Not available

Product Properties

ALogP 5.082
hba_count 3
HBD Count 2
Rotatable Bond 5

Associated Targets(Human)

ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
U2OS (164939 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Mapk1 MAP kinase ERK2 (650 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

Pubchem Sid 504762831
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/504762831
IUPAC Name 4-[8-[(3,4-dimethylphenyl)sulfamoyl]-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-4-yl]benzoic acid
INCHI InChI=1S/C27H26N2O4S/c1-16-6-11-20(14-17(16)2)29-34(32,33)21-12-13-25-24(15-21)22-4-3-5-23(22)26(28-25)18-7-9-19(10-8-18)27(30)31/h3-4,6-15,22-23,26,28-29H,5H2,1-2H3,(H,30,31)
InChIKey XCBONKHCCRJMNW-UHFFFAOYSA-N
Smiles CC1=C(C=C(C=C1)NS(=O)(=O)C2=CC3=C(C=C2)NC(C4C3C=CC4)C5=CC=C(C=C5)C(=O)O)C
Isomeric SMILES CC1=C(C=C(C=C1)NS(=O)(=O)C2=CC3=C(C=C2)NC(C4C3C=CC4)C5=CC=C(C=C5)C(=O)O)C
Molecular Weight 474.57
Reaxy-Rn 36132331
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=36132331&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

6 results found

Lot Number Certificate Type Date Item
I2208106 Certificate of Analysis Jun 09, 2025 M414002
C2303955 Certificate of Analysis Oct 10, 2022 M414002
C2303971 Certificate of Analysis Oct 10, 2022 M414002
C2303954 Certificate of Analysis Oct 10, 2022 M414002
C2303935 Certificate of Analysis Oct 10, 2022 M414002
C2303942 Certificate of Analysis Oct 10, 2022 M414002

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro DMSO: 95 mg/mL (200.18 mM); Ethanol: 41 mg/mL (86.39 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility 95
DMSO(mM) Max Solubility 200.1812167
Water(mg / mL) Max Solubility ＜1
Molecular Weight 474.600 g/mol
XLogP3 5.200
Hydrogen Bond Donor Count 3
Hydrogen Bond Acceptor Count 6
Rotatable Bond Count 5
Exact Mass 474.161 Da
Monoisotopic Mass 474.161 Da
Topological Polar Surface Area 104.000 Ų
Heavy Atom Count 34
Formal Charge 0
Complexity 876.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 3
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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