2531743-46-9
Chemical Structure
GDC-4198
Synonym(s): RGT-419B
- CAS No.: 2531743-46-9
- Formula:C26H30N8O
- Molecular Weight:470.57
InChIKey: QZJWVFBTMGPBPY-IBGZPJMESA-N
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
Biological Activity: 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].
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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. | |||||||||||||||||||||
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- [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.
Keywords
