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Cat. No.: HY-171826

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PROTAC CDK2/4/6 Degrader-1

PROTAC CDK2/4/6 Degrader-1 is an orally active CDK2/CDK4/CDK6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-1 is a prodrug derived from PROTAC CDK2/4/6 Degrader-2 via one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-1 can be used for malignant melanoma research.
(Pink: Aurora A ligand (HY-168440); Blue: Cereblon ligand (HY-10984); Black: linker).

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

CAS No.: 2541626-55-3
Formula: C₄₆H₅₅N₉O₈
Molecular Weight:861.98

Storage:

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

Data Sheet (268 KB)

PROTAC CDK2/4/6 Degrader-1 Chemical Structure

CAS No.: 2541626-55-3

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
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Biological Activity

Description

PROTAC CDK2/4/6 Degrader-1 is an orally active CDK2/CDK4/CDK6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-1 is a prodrug derived from PROTAC CDK2/4/6 Degrader-2 via one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-1 can be used for malignant melanoma research^[1]. (Pink: Aurora A ligand (HY-168440); Blue: Cereblon ligand (HY-10984); Black: linker).

IC₅₀ & Target^[1]

CDK2/cyclinE

CDK6

CDK4

All CDK Isoforms :

All PROTACs Isoforms :

In Vitro

PROTAC CDK2/4/6 Degrader-1 (compound 11) is a prodrug derived from PROTAC CDK2/4/6 Degrader-2 (HY-185121) (compound 3) via one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-2 is a CDK2/CDK4/CDK6 PROTAC degrader degrading CDK2/4/6 proteins and their complexes, inducing cell cycle arrest and apoptosis in melanoma cells^[1].

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

In Vivo

PROTAC CDK2/4/6 Degrader (compound 11) (200 mg/kg, o.p.,once daily for 15 days) distinctly inhibits B16F10 tumor growth and mediate degradation of CDK2/4/6 in B16F10 xenograft mice model^[1].

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

Animal Model:

B16F10 cells induced- C57BL/6J mice^[1]
Dosage:

200 mg/kg
Administration:

o.p., 15 days
Result:

Significantly suppressed tumor sizes.
No Noticeable difference in body weight.

Chemical Information

CAS No. 2541626-55-3
Molecular Weight 861.98
Formula C₄₆H₅₅N₉O₈
SMILES

O=C(C1=CC=C(NC2=NC3=C(C=C(N3C4CCCC4)C(N(C)C)=O)C=N2)C=C1)NCCCCCCNC5=CC=CC(C(N6C7C(N(COC(C(C)(C)C)=O)C(CC7)=O)=O)=O)=C5C6=O
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 (268 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 M, et al. First orally bioavailable prodrug of proteolysis targeting chimera (PROTAC) degrades cyclin-dependent kinases 2/4/6 in vivo. Eur J Med Chem. 2021 Jan 1;209:112903. [Content Brief]

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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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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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PROTAC CDK2/4/6 Degrader-1

All CDK Isoforms

All PROTACs Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC CDK2/4/6 Degrader-1 Related Classifications

HY-171826 Related Classifications