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Cat. No.: HY-138670

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YX-2-177

YX-2-177 is an orally active, selective CDK4/6 inhibitor with IC₅₀ values of 6.1 nM and 14 nM, respectively. YX-2-177 inhibits CDK4/6-mediated Rb phosphorylation. YX-2-177 induces G1 cell cycle arrest and Apoptosis. YX-2-177 can serve as a Target protein ligand to synthesize CDK4/6 PROTAC degraders, such as AC-1-112 (HY-191124). YX-2-177 inhibits breast cancer and non-small cell lung cancer.

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

CAS No.: 1975992-34-7
Formula: C₂₆H₃₀ClN₇O₃
Molecular Weight:524.01

Storage:

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

Data Sheet (285 KB)

YX-2-177 Chemical Structure

CAS No.: 1975992-34-7

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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
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[2]

Cdk4/cyclin D3

6.1 nM (IC₅₀)

cdk6/cyclin D3

14 nM (IC₅₀)

All CDK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
NCI-H1299	IC50	2.49 μM	Antiproliferative activity against human H1299 cells assessed as viability reduction after 3-day incubation by MTT assay. Antiproliferative activity against human H1299 cells assessed as viability reduction after 3-day incubation by MTT assay.	33857728
MDA-MB-231	IC50	1.21 μM	Antiproliferative activity against human MDA-MB-231 breast cancer cells assessed as viability reduction after 3-day incubation by MTT assay. Antiproliferative activity against human MDA-MB-231 breast cancer cells assessed as viability reduction after 3-day incubation by MTT assay.	33857728
MDA-MB-453	IC50	1.75 μM	Antiproliferative activity against human MDA-MB-453 breast cancer cells assessed as viability reduction after 3-day incubation by MTT assay. Antiproliferative activity against human MDA-MB-453 breast cancer cells assessed as viability reduction after 3-day incubation by MTT assay.	33857728
MCF7	IC50	0.38 μM	Antiproliferative activity against human MCF-7 breast cancer cells assessed as viability reduction after 3-day incubation by MTT assay. Antiproliferative activity against human MCF-7 breast cancer cells assessed as viability reduction after 3-day incubation by MTT assay.	33857728

In Vitro

Anti-cancerApoptosisCell Cycle RegulationOthers

Anti-cancer

YX-2-177 (3 days) inhibits the proliferation of MDA-MB-231, MDA-MB-453, MCF-7, and H1299 cells, with IC₅₀ values of 1.21, 1.75, 0.38, and 2.49 μM, respectively^[2].
YX-2-177 (0.1563-2.5 μM; 14 days) inhibits MDA-MB-231 colony formation, with almost no colony formation at 0.625 mM^[2].

Anti-cancer

Apoptosis

YX-2-177 (0.625 µM-10 µM; 24 h) induces apoptosis in MDA-MB-231 cells, with total apoptotic cells reaching 83.02% at 10 mM^[2].

Anti-cancer

Cell Cycle Regulation

YX-2-177 (0.1875-1.50 μM; 12 h) induces G1 phase arrest in MDA-MB-231 cells, increasing the proportion of G1 phase cells to 71.12% at 1.50 mM^[2].
YX-2-177 (0.5-4 µM; 24 h) dose-dependently decreases p-Rb (S780) in MDA-MB-231 cells within the 0.5-4 µM range^[2].

Cell Cycle Regulation

YX-2-177 (Compound C-13) (20-200 nM) inhibits CDK4 and CDK6 with IC₅₀ values of 6.1 nM and 14 nM, respectively, and mean inhibition rates of 95.30% and 93.76% at 200 nM^[2].
YX-2-177 has selective activity against CDK4/CDK6, with IC₅₀ values of 6.1 nM and 14 nM, respectively, superior to other CDKs in the panel^[2].

Others

YX-2-177 (5-20 μM; 72 h) has low cytotoxicity against normal LO2 hepatocytes, with toxicity extending to 20 mM^[2].

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

Cell Viability Assay^[2]

Cell Line:

H1299, MDA-MB-231, MDA-MB-453, and MCF-7
Concentration:

Serial dilutions
Incubation Time:

3 days (exposure); 2 h (MTT)
Result:

IC₅₀ values were 2.49 μM for H1299, 1.21 μM for MDA-MB-231, 1.75 μM for MDA-MB-453, and 0.38 μM for MCF-7.

Cell Cytotoxicity Assay^[2]

Cell Line:

LO2
Concentration:

5-20 μM
Incubation Time:

72 h (exposure); 2 h (MTT)
Result:

Low cytotoxicity was observed toward LO2 cells, with toxicity extending to 20 μM.

Cell Cycle Analysis^[2]

Cell Line:

MDA-MB-231
Concentration:

0.1875, 0.375, 0.75, and 1.50 μM
Incubation Time:

12 h
Result:

G1-phase cells were 68.04% at 0.1875 μM, 68.34% at 0.375 μM, 71.00% at 0.75 μM, and 71.12% at 1.50 μM.
S-phase cells were 15.55%, 15.36%, 11.05%, and 7.55%, respectively.
G2-phase cells were 13.82%, 14.99%, 16.49%, and 19.72%, respectively.

Western Blot Analysis^[2]

Cell Line:

MDA-MB-231
Concentration:

0.5, 1, 2, and 4 µM
Incubation Time:

24 h
Result:

Reduced p-Rb(S780) signal dose-dependently and blocked the CDK4/6→Rb→E2F signaling pathway in MDA-MB-231 cells.

Apoptosis Analysis^[2]

Cell Line:

MDA-MB-231
Concentration:

0.625 µM, 1.25 µM, 2.5 µM, 5 µM, and 10 µM
Incubation Time:

24 h
Result:

Total apoptotic cells were 8.06% at 0.625 µM, 17.51% at 1.25 µM, 48.74% at 2.5 mM, 71.34% at 5 mM, and 83.02% at 10 mM.
Early apoptotic cells increased from 4.24% at 0.625 µM to 68.48% at 10 mM.

In Vivo

Anti-cancer

YX-2-177 (40-80 mg/kg/d; p.o.; daily; 21 days) produces dose-dependent tumor growth inhibition in MDA-MB-231 xenografts, with TGI of 93.49% at 40 mg/kg and 104.68% at 80 mg/kg^[2].

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

Animal Model:

BALB/c nude (female, 6-7 weeks old)^[2]
Dosage:

40 mg/kg/d; 80 mg/kg/d
Administration:

p.o.; daily; 21 days
Result:

Tumor growth inhibition (TGI) was 93.49% at 40 mg/kg and 104.68% at 80 mg/kg in the MDA-MB-231 xenograft model.
Tumor volume and mass were reduced in a dose-dependent manner.

Related Protocols :

Chemical Information

CAS No. 1975992-34-7
Molecular Weight 524.01
Formula C₂₆H₃₀ClN₇O₃
SMILES

O=C1C(C(C)=O)=C(C)C2=CN=C(NC3=NC=C(N4CCN(C(CCl)=O)CC4)C=C3)N=C2N1C5CCCC5
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 (285 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]. Joseph Salvino, et al. Proteolysis-targeting chimeras. WO2020092662A1. WIPO (PCT). 2019-10-30.

[2]. Shan H, et al. Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold. Eur J Med Chem. 2021 Jul 5;219:113432. [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.

Bioz

MOQ

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100 mg

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

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YX-2-177

All CDK Isoforms