2. Cell Cycle/DNA Damage
  3. CDK
  4. GDC-4198

GDC-4198 (RGT-419B) is an orally active CDK4/2 inhibitor with desired degrees of selectivity against kinases such as CDK6, CDK9 and GSK3β. GDC-4198 inhibits the activity of cyclin-CDK complexes, blocks phosphorylation of the retinoblastoma protein (pRb), arresting the cell cycle transition from G1 to S phase. GDC-4198 is promising for research of cancers, such as breast cancer (especially hormone receptor-positive, HER2-negative type), lung cancer, and colorectal cancer.

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

GDC-4198

GDC-4198 Chemical Structure

CAS No. : 2531743-46-9

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Based on 1 publication(s) in Google Scholar

GDC-4198 Related Antibodies

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Description

GDC-4198 (RGT-419B) is an orally active CDK4/2 inhibitor with desired degrees of selectivity against kinases such as CDK6, CDK9 and GSK3β. GDC-4198 inhibits the activity of cyclin-CDK complexes, blocks phosphorylation of the retinoblastoma protein (pRb), arresting the cell cycle transition from G1 to S phase. GDC-4198 is promising for research of cancers, such as breast cancer (especially hormone receptor-positive, HER2-negative type), lung cancer, and colorectal cancer[1][2][3].

IC50 & Target[1][2]

CDK4

 

CDK2

 

In Vitro

In vitro, GDC-4198 shows more robust activity against Palbociclib-resistant ER+ breast cancer cells than abemaciclib. In ER+ T47D breast cancer cells with overexpression of Cyclin E1, GDC-4198 exhibits antiproliferation activity[1].

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

GDC-4198 Related Antibodies
In Vivo

GDC-4198 demonstrates in vivo tumor growth inhibition in an ER+ breast cancer xenograft model[1].

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

470.57

Formula

C26H30N8O
CAS No.
SMILES

CC(C1=C2N(N=C1)C=CC(C3=NC(NC4=CC=C(N5C(C[C@H](CC5)N(C)C)=O)C=N4)=NC=C3)=C2)C
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
References
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GDC-4198 Related Classifications

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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.

Keywords:

GDC-41982531743-46-9RGT-419BGDC4198GDC 4198CDKCyclin dependent kinaseCDK2CDK4CDK6pRbcancersInhibitorinhibitorinhibit

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