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RMC-6291 is an Orally Active and Covalent KRASG12C Inhibitor for Solid Tumor Research

Louis Gilman April 26, 2023

KRAS  plays a critical role in regulating cell growth and division. KRAS mutations are common in many types of solid tumors, including lung, colon, and pancreatic cancers, and are associated…

Cancer Colorectal Cancer Lung Adenocarcinoma Lung Cancer NSCLC

Sotorasib (AMG-510) is an Orally Bioavailable KRAS G12C Covalent Inhibitor

Louis Gilman March 10, 2023

The KRAS oncoprotein is a GTPase and an essential mediator of intracellular signaling pathways. KRAS oncoprotein regulates tumor cell growth and survival. However, KRAS also is the most frequently mutated…

Cancer

GNE-9815 is a highly selective pan-RAF inhibitor, can be used to research KRAS mutant cancers

Louis Gilman October 24, 2022

Rapidly accelerated fibrous sarcoma (RAF) kinases are a family of three serine/threonine-specific protein kinases associated with retroviral oncogenes. They play key roles in several cellular processes, including cell cycle progression,…

Pancreas Cancer

IACS-15414 is an Orally Active SHP2 Inhibitor

Louis Gilman January 31, 2022

Src-homology-2-containing protein tyrosine phosphatase 2 (SHP2), encoded by the PTPN11 gene, is a classical nonreceptor protein tyrosine phosphatase (PTP). SHP2 is a ubiquitous protein tyrosine phosphatase with a relatively conserved…

Lung Cancer Lymphoma Non-Small Cell Lung Cancer

Repotrectinib is a potent ROS1 and TRK Inhibitor

Louis Gilman January 3, 2022

Repotrectinib is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. The IC50 values are 0.83/0.05/0.1 nM for TRKA/B/C, respectively. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib inhibits mutant ALKs. It inhibits…

Breast Cancer Triple-Negative Breast Cancer

LJI308 is a Pan-Ribosomal S6 Kinase (RSK) Inhibitor

Louis Gilman June 2, 2021

The cold shock protein Y-box binding protein-1 (YB-1) is a multifunctional protein. It shows relations in cell proliferation, survival, and stress response. Through translation and transcription of key proteins and…

Abdominal Aortic Aneurysm Lung Cancer Prostate Cancer

SMAP-2 (DT-1154) is an Orally Bioavailable PP2A Activator

Louis Gilman June 1, 2021

Protein Phosphatase 2A (PP2A) is a serine/threonine phosphatase. It regulates multiple signaling cascades implicated in cancer progression, including downstream effectors of KRAS. Inhibition of PP2A contributes to oncogenesis in multiple…

Lung Adenocarcinoma Lung Cancer Non-Small Cell Lung Cancer

DT-061 is an Orally Active PP2A Activator

Louis Gilman May 21, 2021

Protein phosphatase 2A (PP2A) comprises a family of serine/threonine phosphatases, minimally containing a well-conserved catalytic subunit. PP2A plays a prominent role in the regulation of specific signal transduction cascades. Additionally,…

Cancer

BI-3406 is an Orally Active and Selective KRAS and SOS1 Interaction Inhibitor

Louis Gilman May 18, 2021

KRAS functions as a molecular switch, cycling between inactive (GDP-bound) and active (GTP-bound) states to transduce extracellular signals via cell-surface receptors. KRAS signaling occurs through engagement with effector proteins that…

Colorectal Cancer Lung Cancer Non-Small Cell Lung Cancer Ovary Cancer Pancreas Cancer

Rineterkib is an Orally Active RAF and ERK1/2 Inhibitor

Louis Gilman April 1, 2021

ERK1 and ERK2 are related protein-serine/threonine kinases that participate in the Ras-Raf-MEK-ERK signal transduction cascade. This cascade participates in the regulation of a large variety of processes. It includes cell…

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OATD-02 is an Orally Active Arginase 1/2 Inhibitor for Melanoma Research

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INCB086550 is an Orally Active PD-L1 Inhibitor for Multiple Cancers Research

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