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Cat. No.: HY-133617

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PROTAC CDK9 degrader-14

PROTAC CDK9 degrader-14 is a CDK9 PROTAC degrader that recruits CRBN. PROTAC CDK9 degrader-14 efficiently degrades CDK9 and inhibits cell proliferation in solid tumors and hematological malignancies. PROTAC CDK9 degrader-14 can be used in research related to solid tumors, hematological malignancies and triple-negative breast cancer.
(Pink: CDK9 ligand (HY-150946); Blue: Cereblon ligand (HY-138793); Black: linker).

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

CAS No.: 2411019-98-0
Formula: C₄₂H₅₃N₉O₆
Molecular Weight:779.93

Storage:

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

PROTAC CDK9 degrader-14 Chemical Structure

CAS No.: 2411019-98-0

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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

PROTAC CDK9 degrader-14 is a CDK9 PROTAC degrader that recruits CRBN. PROTAC CDK9 degrader-14 efficiently degrades CDK9 and inhibits cell proliferation in solid tumors and hematological malignancies. PROTAC CDK9 degrader-14 can be used in research related to solid tumors, hematological malignancies and triple-negative breast cancer^[1]^[2]. (Pink: CDK9 ligand (HY-150946); Blue: Cereblon ligand (HY-138793); Black: linker).

IC₅₀ & Target

^[1]

CDK9

All PROTACs Isoforms :

All CDK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-468	IC₅₀	0.104 μM	Antiproliferative activity against human MDA-MB-468 triple-negative breast cancer cells assessed via cell growth inhibition assay following standard incubation protocols. Antiproliferative activity against human MDA-MB-468 triple-negative breast cancer cells assessed via cell growth inhibition assay following standard incubation protocols.	34538051
BT-549	IC₅₀	0.04 μM Compound: 35	Growth inhibition of human BT-549 cells assessed as cell viability measured after 4 days by WST8 assay Growth inhibition of human BT-549 cells assessed as cell viability measured after 4 days by WST8 assay	[PMID: 34538051]
BT-549	IC₅₀	0.040 μM	Antiproliferative activity against human BT549 triple-negative breast cancer cells assessed via cell growth inhibition assay following standard incubation protocols. Antiproliferative activity against human BT549 triple-negative breast cancer cells assessed via cell growth inhibition assay following standard incubation protocols.	34538051
MDA-MB-231	IC₅₀	0.072 μM Compound: 35	Growth inhibition of human MDA-MB-231 cells assessed as cell viability measured after 4 days by WST8 assay Growth inhibition of human MDA-MB-231 cells assessed as cell viability measured after 4 days by WST8 assay	[PMID: 34538051]
MDA-MB-231	IC₅₀	0.072 μM	Antiproliferative activity against human MDA-MB-231 triple-negative breast cancer cells assessed via cell growth inhibition assay following standard incubation protocols. Antiproliferative activity against human MDA-MB-231 triple-negative breast cancer cells assessed via cell growth inhibition assay following standard incubation protocols.	34538051
MDA-MB-468	IC₅₀	0.104 μM Compound: 35	Growth inhibition of human MDA-MB-468 cells assessed as cell viability measured after 4 days by WST8 assay Growth inhibition of human MDA-MB-468 cells assessed as cell viability measured after 4 days by WST8 assay	[PMID: 34538051]

In Vitro

PROTAC CDK9 degrader-14 (compound C025) (0.01-2.5 μM) potently and selectively degrades CDK9 protein in cultured mammalian cells, with no significant effect on the protein levels of CDK1, CDK2, CDK4 or CDK5^[1].
PROTAC CDK9 degrader-14 (compound 35) potently inhibits the proliferation of triple-negative breast cancer (TNBC) cells MDA-MB-468, BT549 and MDA-MB-231, with an IC₅₀ range of 0.040-0.104 μM^[2].

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

Western Blot Analysis^[2]

Cell Line:

MDA-MB-231
Concentration:

500 nM
Incubation Time:

8 h
Result:

Induced degradation of CDK9.

Chemical Information

CAS No. 2411019-98-0
Molecular Weight 779.93
Formula C₄₂H₅₃N₉O₆
SMILES

O=C1C2=C(CN1C3CCC(NC3=O)=O)C(OCCCCCCCC(NC4=CC=C(CNC5=NC(OC6CCN(CC6)C)=NC7=C(C(C)C)C=NN57)C=C4)=O)=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

Handling Instructions (2659 KB)

References

[1]. Chen, X, et al. Degradation agents for cyclin dependent kinase, preparation method thereof, pharmaceutical composition thereof and use thereof. WO2020035049A1. WIPO. 20.02.2020.

[2]. Wei D, et al. Discovery of Potent and Selective CDK9 Degraders for Targeting Transcription Regulation in Triple-Negative Breast Cancer. Journal of medicinal chemistry. 2021 Oct 14;64(19):14822-14847. [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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