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Cat. No.: HY-139996

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Pomalidomide-C5-Dovitinib

Pomalidomide-C5-Dovitinib is a heterobifunctional PROTAC that recruits KEAP1 E3 ligase to degrade BRD4 and BRD3, but not BRD2.
(Pink: c-Kit and FLT3 ligand (HY-50905); Blue: Cereblon ligand (HY-130737); Black: linker (HY-B0236)).

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

CAS No.: 2732969-67-2
Formula: C₃₉H₃₈FN₉O₆
Molecular Weight:747.77

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (275 KB)

Pomalidomide-C5-Dovitinib Chemical Structure

CAS No.: 2732969-67-2

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

Pomalidomide-C5-Dovitinib is a heterobifunctional PROTAC that recruits KEAP1 E3 ligase to degrade BRD4 and BRD3, but not BRD2^[1]. (Pink: c-Kit and FLT3 ligand (HY-50905); Blue: Cereblon ligand (HY-130737); Black: linker (HY-B0236)).

IC₅₀ & Target

^[1]

BRD3

BRD4

All PROTACs Isoforms :

All Epigenetic Reader Domain Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MOLM-13	IC₅₀	9.5 nM Compound: 2	Antiproliferative activity against human MOLM-13 cells incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human MOLM-13 cells incubated for 48 hrs by CCK-8 assay	[PMID: 34694800]
MV4-11	IC₅₀	9.2 nM Compound: 2	Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by CCK-8 assay	[PMID: 34694800]

In Vitro

KEAP1 E3 ligase refers to the substrate recognition subunit of the Cullin 3 (RING) type E3 ubiquitin ligase complex. It regulates cellular oxidative stress responses and antioxidant defense pathways by recognizing and ubiquitinizing substrate proteins such as NRF2. Mutations in cancer often lead to loss of function.

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

Chemical Information

CAS No. 2732969-67-2
Molecular Weight 747.77
Formula C₃₉H₃₈FN₉O₆
SMILES

O=C1NC2=C(C(N)=C1C3=NC4=CC=C(N5CCN(CC5)C(CCCCCNC6=CC=CC(C(N7C8C(NC(CC8)=O)=O)=O)=C6C7=O)=O)C=C4N3)C(F)=CC=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Wei J, et al. Harnessing the E3 Ligase KEAP1 for Targeted Protein Degradation. Journal of the American Chemical Society. 2021 Sep 22;143(37):15073-15083. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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