PeptideDB

TC11 100823-03-8

TC11 100823-03-8

CAS No.: 100823-03-8

TC11 is an MCL1 degrader and activator of Caspase-9 and CDK1. TC11 is a phthalimide analogue that is structurally relate
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TC11 is an MCL1 degrader and activator of Caspase-9 and CDK1. TC11 is a phthalimide analogue that is structurally related to immunomodulatory active molecules. During prolonged mitotic arrest, TC11 induces MCL1 degradation leading to apoptotic death.

Physicochemical Properties


Molecular Formula C20H22N2O2
Molecular Weight 322.40
Exact Mass 322.168
CAS # 100823-03-8
PubChem CID 1235479
Appearance White to yellow solid powder
LogP 4.962
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 3
Rotatable Bond Count 3
Heavy Atom Count 24
Complexity 486
Defined Atom Stereocenter Count 0
InChi Key NRPIRIUWEKTNGQ-UHFFFAOYSA-N
InChi Code

InChI=1S/C20H22N2O2/c1-11(2)14-6-5-7-15(12(3)4)18(14)22-19(23)16-9-8-13(21)10-17(16)20(22)24/h5-12H,21H2,1-4H3
Chemical Name

5-amino-2-[2,6-di(propan-2-yl)phenyl]isoindole-1,3-dione
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.
Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


Targets CDK1 Caspase-9 MCL1
ln Vitro In KMS34 cells, TC11 (0~30 μM; 24 hours) causes cell death[1]. TC11 (5 μM; 0~48 hours; KMS34 cells) causes M arrest and downregulates MCL1 expression as well as an apoptotic pathway that leads to cell death[1].
Cell Assay Cell Viability Assay[1]
Cell Types: KMS34 cells
Tested Concentrations: 0~30 μM
Incubation Duration: 24 hrs (hours)
Experimental Results: Induced cell death.

Western Blot Analysis[1]
Cell Types: KMS34 cells
Tested Concentrations: 5 μM
Incubation Duration: 0~48 hrs (hours)
Experimental Results: Induced cell death occurs through an apoptotic pathway and downregulated MCL1 expression.

Cell Cycle Analysis[1]
Cell Types: KMS34 cells
Tested Concentrations: 5 μM
Incubation Duration: 24 hrs (hours)
Experimental Results: Induced M arrest.
References

[1]. A phenylphthalimide derivative, TC11, induces apoptosis by degrading MCL1 in multiple myeloma cells. Biochem Biophys Res Commun. 2020;521(1):252-258.

[2]. A phthalimide derivative that inhibits centrosomal clustering is effective on multiple myeloma. PLoS One. 2012;7(6):e38878.


Solubility Data


Solubility (In Vitro) DMSO : 50 mg/mL (155.09 mM)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 2.5 mg/mL (7.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.1017 mL 15.5087 mL 31.0174 mL
5 mM 0.6203 mL 3.1017 mL 6.2035 mL
10 mM 0.3102 mL 1.5509 mL 3.1017 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.