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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
54 Results for "
KRASG12C
" in MedChemExpress (MCE) Product Catalog:
Products (54)
54 Results for "KRASG12C" in MCE Product Catalog:
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Divarasib (GDC-6036) adipate is an orally active, selective KRASG12C inhibitor with an IC50 of <0.01 μM. Divarasib adipate covalently binds Cys12 in GDP-bound KRASG12C, occupies the switch II pocket, blocks GTP binding and SOS-mediated reactivation, and inhibits oncogenic KRAS signaling. Divarasib adipate induces tumor shrinkage and robust tumor growth inhibition in KRASG12C-positive models and cancer cells. Divarasib adipate can be used for the research of non-small cell lung cancer, colorectal adenocarcinoma, pancreatic ductal adenocarcinoma, and other KRASG12C-mutated solid tumors .
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Elironrasib is an orally active and covalent inhibitor of KRAS G12C(ON). Elironrasib forms a tri-complex within tumor cells between KRAS G12C(ON) and cyclophilin A (CypA). Thus, Elironrasib prevents KRAS G12C(ON) from signaling via steric blockade of RAS effector binding. Elironrasib inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. Elironrasib also inhibits the proliferation of KRAS G12C mutant cells with a median IC50 of 0.11 nM .
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2 Cited Publications
Research Areas:
MRTX0902 is a potent, selective, brain-penetrant, and orally active SOS1 inhibitor with a Ki of 1.9 nM. MRTX0902 disrupts the SOS1:KRASG12C protein-protein interaction (PPI). MRTX0902 can be used in research on pancreatic ductal adenocarcinoma .
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1 Cited Publications
Cat. No.: HY-18707
CAS No.: 1469337-95-8
K-Ras(G12C) inhibitor 12 is an irreversible inhibitor of K-Ras(G12C). K-Ras(G12C) inhibitor 12 can alter the nucleotide-binding preference of K-Ras and block its interaction with effector proteins. K-Ras(G12C) inhibitor 12 can reduce cell viability and induce apoptosis in lung cancer cell lines with G12C mutations. K-Ras(G12C) inhibitor 12 has anti-tumor activity .
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) .
BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
Cat. No.: HY-164493
CAS No.: 2409131-50-4
KRASG12C IN-13 (LY3499446) is a potent KRAS G12C inhibitor. KRASG12C IN-13 is promising for research of advanced solid tumors including non-small cell lung cancer and colorectal cancer .
Cat. No.: HY-153262
CAS No.: 2706637-12-7
Synonyms: (7R)-D3S-001
KRASG12C IN-2 (compound 17) is an orally active KRAS G12C inhibitor. KRASG12C IN-2 inhibits tumor growth in mice .
Cat. No.: HY-176811
CAS No.: 3055318-88-9
VVD-442 is an inhibitor targeting PI3Kα. VVD-442 covalently binds to Cys242 in the RAS-binding domain of PI3K p110α, induces conformational changes, and disrupts the interaction between PI3K p110α and RAS proteins. VVD-442 also blocks RAS-mediated PI3K activation. VVD-442 can be used in research related to RAS-mutant cancers and HER2-overexpressing cancers .
Cat. No.: HY-155356
YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.
Cat. No.: HY-173252
Research Areas:
KRASG12C ligand-1 is a PROTAC target protein ligand that can be used to synthesize the PROTAC YN14-H (HY-173250). YN14-H is a PROTAC degrader targeting KRAS G12C and has antitumor activity .
MRTX849 analog 24 is a KRAS G12C inhibitor with a human IC50 of 140 nM. MRTX849 analog 24 binds to KRAS G12C, forms a covalent interaction, and acts as a click probe to bait the protein target in proteomic studies. MRTX849 analog 24 exhibits cellular activity in cancer cells. MRTX849 analog 24 can be used for the research of kras G12C-mutant cancer .
Cat. No.: HY-179403
CAS No.: 2966924-23-0
KRASG12C IN-17 is an orally active covalent KRAS G12C inhibitor, showing strong inhibitory activity in KRAS G12C-mutant cancer cells (NCI-H23 IC50 = 0.7 nM; NCI-H358 IC50 = 0.5 nM).
KRASG12C IN-17 covalently and irreversibly binds to KRAS G12C with > 96% modification efficiency in both GDP-bound and GMPPNP-bound conformations.
KRASG12C IN-17 can be used for studies of KRAS-driven cancers, including colorectal cancer .
Cat. No.: HY-12446
CAS No.: 1469337-91-4
K-Ras (G12C) inhibitor 9 is an allosteric inhibitor of the K-Ras (G12C) .
Cat. No.: HY-146223
Purity: 99.52%
AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase KRASG12C inhibitor with an IC50 of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRASG12C mutations. AZD4625 can be used for the study of KRASG12C mutant non-small cell lung cancer .
Cat. No.: HY-182883
KRASG12C IN-20 is an orally potent KRAS G12C inhibitor with an EC50 of 3.9 nM. KRASG12C IN-20 covalently modifies KRAS G12C in its inactive GDP-bound state and locks it to block oncogenic signal transduction. KRASG12C IN-20 exhibits significant activity in lung adenocarcinoma xenograft models. KRASG12C IN-20 can be used for research related to lung adenocarcinoma .
Cat. No.: HY-175583
CAS No.: 2725905-93-9
Research Areas:
KRASG12C ligand-2 is a KRas ligand used for PROTAC synthesis. KRASG12C ligand-2 serves as the target protein ligand of PROTAC KRAS G12C degrader-2 (HY-153821) .
Target:
Research Areas:
(R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
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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
