2. PROTAC
  3. E3 Ligase Ligand-Linker Conjugates
  4. Thalidomide-NH-C6-NH-Boc

Thalidomide-NH-C6-NH-Boc 

Cat. No.: HY-130854 Purity: 96.11%
COA Handling Instructions

Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A).

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

Thalidomide-NH-C6-NH-Boc Chemical Structure

Thalidomide-NH-C6-NH-Boc Chemical Structure

CAS No. : 2093536-13-9

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Based on 1 publication(s) in Google Scholar

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von Hippel-Lindau (VHL) MDM2 Cereblon cIAP1

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Description

Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A)[1].
IC50 & Target[1]

Cereblon

 

In Vitro

MI-389 (0-1 μM; 72 hours) decreases cell growth with an EC50 value of 21.3 nM, which is comparable to the cellular potency of sunitinib (EC50=17.3 nM)[1].
MI-389 (0-500 nM; 72 hours) leads to GSPT1 destabilization fastly as a dosepdependent manner. It shows a complete GSPT1 depletion at 100 nM[1].

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

Cell Viability Assay[1]

Cell Line: Kasumi-1 cells (a c-KIT dependent acute myeloid leukemia (AML) cell line); GIST-T1
Concentration: 0-1 μM
Incubation Time: 72 hours
Result: Outperform decreased-antiproliferative effect than sunitinib

Western Blot Analysis[1]

Cell Line: Kasumi-1 cells (a c-KIT dependent acute myeloid leukemia (AML) cell line); GIST-T1
Concentration: 1 nM, 5 nM, 10 nM, 50 nM, 100 nM, 500 nM
Incubation Time: 4 hours
Result: Decreased GSPT-1 protein expression.
Molecular Weight

472.53

Appearance

Solid

Formula

C24H32N4O6
CAS No.
SMILES

O=C(OC(C)(C)C)NCCCCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (211.63 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1163 mL 10.5813 mL 21.1627 mL
5 mM 0.4233 mL 2.1163 mL 4.2325 mL
10 mM 0.2116 mL 1.0581 mL 2.1163 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (5.29 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Thalidomide-NH-C6-NH-Boc2093536-13-9E3 Ligase Ligand-Linker ConjugatesMI389PROTACKasumi-1leukemiaAMLT-AMLCCRF-CEMJURKATMOLT4Inhibitorinhibitorinhibit

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