GDC-4198  (Synonyms: RGT-419B)

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].

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 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.

470.57

C₂₆H₃₀N₈O

2531743-46-9

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

Room temperature in continental US; may vary elsewhere.

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

• [1]. Zhi Xie, et al. Abstract PS16-22: Targeting resistance to current CDK4/6 therapies by RGT-419B, an inhibitor with optimized kinase activity spectrum. Cancer Res (2021) 81 (4_Supplement): PS16-22.

  [2]. Zhilong Hu, et al. Cdk inhibitors. WO2020224568A1. 2020-11-12.

  [3]. Xiaotian Zhu, et al. Salt and solid forms of a cdk inhibitor. WO2025103447A1. 2025-05-22.