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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
320 Results for "
KRAS+G12
" in MedChemExpress (MCE) Product Catalog:
Products (320)
320 Results for "KRAS+G12" in MCE Product Catalog:
Cat. No.: HY-185205
CAS No.: 3055745-21-3
VVD-484 is a PI3K p110α inhibitor with an IC50 of 0.59 μM against human targets.,VVD-484, classified as a "silent ligand", forms a covalent bond with Cys242 of PI3K p110α without disrupting the p110α-KRAS G12C interaction. VVD-484 inhibits phosphorylation (S473) of AKT via a RAS-independent pathway. VVD-484 can be used in the research of HER2-overexpressing cancers .
Cat. No.: HY-175244
Target:
Research Areas:
SOS1-IN-20 (Compound 12f) is an orally active SOS1 inhibitor with an IC50 of 5.11 nM against KRAS G12C::SOS1. By disrupting the interaction between KRAS and SOS1, SOS1-IN-20 inhibits KRAS activation and downstream signal transduction. SOS1-IN-20 has an IC50 of 253 nM for p-ERK in PC-9 cells and 16.71 μM for hERG channel . SOS1-IN-20 can inhibit the proliferation of tumor cells and has antitumor activity .
Cat. No.: HY-P705030
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: HLA-A*0301 & B2M & KRASG12D (VVVGADGVGK)
Cat. No.: HY-P705319
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: HLA-A*0201 & B2M & KRASG12C (KLVVVGACGV)
Cat. No.: HY-P705320
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: HLA-A*0201 & B2M & KRASG12D (KLVVVGADGV)
Cat. No.: HY-P705321
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: HLA-A*0201 & B2M & KRASG12V (KLVVVGAVGV)
Cat. No.: HY-P705322
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: HLA-A*0201 & B2M & KRASG12V (VVVGAVGVGK)
Cat. No.: HY-P705349
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: HLA-A*0301 & B2M & KRASG12C (VVGACGVGK)
Cat. No.: HY-P705350
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: HLA-A*0301 & B2M & KRASG12C (VVVGACGVGK)
Cat. No.: HY-P705357
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: HLA-A*1101 & B2M & KRASG12V (VVVGAVGVGK)
Cat. No.: HY-174243
CAS No.: 2933935-13-6
KRASG12D-IN-5 (Compound 241) is an orally active KRAS(G12D) inhibitor with an IC50 of 11 nM. KRASG12D-IN-5 has potent anticancer activity with no significant cytotoxicity against BxPC-3 (WT), KRAS mutation AsPC-1 (G12D) and MIAPaCa-2 cells (G12C) with CC50s of 10.37, 0.76 and 0.3 μM, respectively. KRASG12D-IN-5 can be used for cancer research, such as lung, pancreatic and colorectal cancer .
Cat. No.: HY-P992366
Cat. No.: HY-168012
CAS No.: 3054023-07-0
Target:
Research Areas:
Pan-RAS-IN-6 (compound 24) is an inhibitor targeting DUSP6, which reduces MAPK activation in the brain of the NCI-H1373-Luc model (DUSP6), at the same time, it shows significant tumor growth inhibition and tumor regression effects in the NSCLC brain metastasis mouse model. Pan-RAS-IN-6 shows high selectivity and strong inhibitory effects, especially in KRAS mutation-related signaling pathways, demonstrating varying inhibitory activity against different KRAS mutants and interacting proteins. The IC50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively .
Cat. No.: HY-P2265A
CAS No.: 2896737-31-6
Synonyms: HL-085
Tunlametinib is a highly selective, orally active MEK1/2 inhibitor (IC50=1.9 nM, MEK1). Tunlametinib blocks the RAS-RAF-MEK-ERK signaling pathway, arrests tumor cell cycle and promotes apoptosis. Tunlametinib potently inhibits the proliferation of RAS/RAF mutant cancer cells (such as BRAF V600E, KRAS G12C mutant cells). Tunlametinib shows synergistic anti-tumor effects with BRAF/KRASG12C/SHP2 inhibitors, Docetaxel (HY-B0011). Tunlametinib can be used to study targeted therapy for RAS/RAF mutation-driven malignancies (such as melanoma, colorectal cancer, and non-small cell lung cancer) .
Cat. No.: HY-176786
CAS No.: 3104382-00-2
MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader without affecting KRAS transcription. MCB-36 exhibits minimal effects on HRAS and NRAS protein levels. MCB-36 binds to the GDP-loaded state of G12D, G12C, G12V, and wild-type KRAS with high affinities Kd ≈ 1 pM). MCB-36 decreases p-ERK levels, leading to cell apoptosis. MCB-36 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-36 can be used for the study of colorectal cancer and lung cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-112078); Black: Linker (HY-W091879)) .
Cat. No.: HY-176785S
Cat. No.: HY-175870A
CAS No.: 3024878-21-2
(7R)-Eras-4001 is an orally active KRAS mutant inhibitor with remarkable selectivity for H-RAS and N-RAS. (7R)-Eras-4001 effectively suppresses cancer cell viability by blocking downstream signaling pathways mediated by RAF family proteins, inhibiting the formation of the KRAS G12D-RAF1 RBD complex and the phosphorylation of ERK1/2. (7R)-Eras-4001 induces tumor growth inhibition and regression in a dose-dependent manner, and also reduces plasma ERK1/2 phosphorylation levels. (7R)-Eras-4001 exerts a synergistic effect with anti-PD-1 Cetuximab (HY-P9905). (7R)-Eras-4001 can be used in research on non-small cell lung cancer, pancreatic cancer, colorectal cancer, and ovarian cancer .
Cat. No.: HY-L260
75 compounds
KRAS (Kirsten Rat Sarcoma Viral Oncogene Homolog) is one of the most important oncogenic driver genes in oncology, with high mutation frequencies in pancreatic cancer, non‑small cell lung cancer, and colorectal cancer. For a long time, KRAS was considered "undruggable" due to the lack of suitable small‑molecule binding pockets on its protein surface. In recent years, with the discovery of the switch‑II pocket and the successful approval of KRAS G12C inhibitors, KRAS‑targeted research has achieved groundbreaking progress, which has also spurred a wave of development targeting non‑G12C mutants such as G12D and G12V, as well as upstream and downstream regulatory factors including SOS1 and SHP2.
MCE KRAS Targeted Compound Library contains 75 small‑molecule compounds targeting the KRAS, serving as high‑quality research tools for mechanistic studies of KRAS‑mutant tumors, combination therapy development, resistance mechanism exploration, and high‑throughput drug screening, thereby providing robust support for KRAS‑targeted drug discovery.
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
