g12v

Rineterkib (ERK-IN-1) is an inhibitor of RAF and ERK1/2 activating mutations in the MAPK pathway.

KRAS G12V Peptide TFA is the trifluoroacetic acid salt form of KRAS G12V Peptide. This specific peptide is derived from the Kirsten rat sarcoma virus (KRAS) gene harboring the oncogenic G12V mutation. KRAS G12V Peptide induces responses such as IFN-γ secretion and cytotoxicity. It is utilized in studies of immune responses against tumors with the KRAS G12V mutation.

KRAS G12V Peptide is a specific peptide derived from the Kirsten rat sarcoma virus (KRAS) gene carrying the G12V oncogenic mutation. It induces responses such as IFN-γ secretion and cytotoxicity, making it useful for studying immune responses against tumors with the KRAS G12V mutation.

BI-2493 is a highly selective pan-KRAS inhibitor and structural analog of BI-2865.BI-2493 exhibits antitumor activity and inhibits tumor cell growth and can be used in the study of cancerous diseases.BI-2493 is a highly selective pan-KRAS inhibitor and structural analog of BI-2865.

Daraxonrasib (RMC-6236) is an orally effective and novel triple complex RAS (ON) MULTI inhibitor, which is a potent non covalent inhibitor of multiple RAS variants in GTP binding state. RMC-6236 has anti-tumor activity and can be used in research related to RAS driven tumors. With rich experience in compound synthesis, we can provide fast customized synthesis services for this product according to your research needs.

BI-2865 is a non-covalent pan-KRAS inhibitor.BI-2865 binds to KRAS WT, G12C, G12D, G12V, and G13D mutants with KD values of 6.9, 4.5, 32, 26, and 4.3 nM, respectively.BI-2865 showed antiproliferative activity in BaF3 cells expressing KRAS G12C, G12D, or G12V mutants[1] . BI-2865 showed antiproliferative activity on BaF3 cells expressing KRAS G12C, G12D or G12V mutants, with an average IC50 value of approximately 140 nM.[1]

AMG410 is a non-covalent, dual-modality KRAS inhibitor effective against both GDP (OFF) and GTP (ON) binding, with Kd (GDP) of 1 nM and Kd (GTP) of 22 nM, capable of blocking KRAS independently of the cell cycle. AMG410 does not affect HRAS and NRAS2, and exhibits high potency against KRAS G12D, G12V, G12C, G13D, and other mutants, with an IC₅₀ of 1–4 nM. It induces tumour regression and reduces phosphorylated ERK levels in KRAS-mutant cancer models.

KRAS inhibitor-31 (compound 33), a potent agent targeting KRAS, exhibits K D (SPR) values of 0.019 nM for KRas G12D, 0.019 nM for KRas G12C, and 0.096 nM for KRas G12V, illustrating its efficacy across these variants.

pan-KRAS degrader 1 is a pan-KRAS inhibitor with IC50 values of 29 nM and 9 nM against wild-type KRAS and G12V mutant respectively. It exerts anti-proliferative effects in KRAS-mutant cell lines and is suitable for lung cancer research.

KRAS inhibitor-37 (compound 2) is a potent inhibitor of KRAS, exhibiting low dissociation constants (KD) with various KRAS mutations: wild type (0.004 nM), G12D (0.041 nM), G12C (0.019 nM), and G12V (0.144 nM). This compound effectively inhibits cell proliferation, demonstrating half-maximal inhibitory concentrations (IC50) ranging from <2 nM to 14 nM in H358, SW620, and PANC08.13 cell lines. KRAS inhibitor-37 holds potential for cancer research applications.

PROTAC K-Ras degrader-2 (compound 48) is a broad-spectrum KRAS mutant PROTAC degrader that demonstrates an IC50 of ≤200 nM for KRAS G12V/RAF1. Additionally, PROTAC K-Ras degrader-2 achieves a DC50 of ≤200 nM in degrading SW620 KRAS G12D and inhibits the growth of SW620 3D cells with an IC50 of ≤20 nM.

pan-KRAS-IN-13 (compound 2) is a potent inhibitor of KRAS, exhibiting IC50 values of 2.75 nM and 2.89 nM for its G12D and G12V mutations, respectively.

KRAS-IN-43 (Compound 9) is a broad-spectrum KRAS inhibitor with IC50 values of 0.15 μM for KRASG12V, 0.14 μM for KRASG12C, and 0.47 μM for wild-type KRAS. It disrupts the interaction between KRAS and cRAF and suppresses ERK phosphorylation. KRAS-IN-43 shows potential for research in KRAS mutation-associated cancers, including pancreatic, colorectal, and lung cancers.

KRAS-IN-51 (Compound 597a) is a KRas G12V inhibitor with an IC50 of 2.9 nM for KRas G12V. It has KD values of 17 nM at 20°C and 68 nM at 37°C. KRAS-IN-51 inhibits the phosphorylation of pERK and exhibits antiproliferative activity against SW620 and MIAPaCa-2 cell lines. This compound is applicable for research in colorectal cancer and pancreatic cancer.

BBO-11818 is an orally active, non-covalent pan-KRAS inhibitor that simultaneously targets both the inactivated and activated forms of the KRAS protein, inhibiting a wide range of oncogenic mutants. BBO-11818 significantly inhibits the MAPK/ERK signaling pathway and the proliferation of KRAS-mutated tumor cells. It is currently being evaluated in the KONQUER-101 Phase I clinical trial for the treatment of KRAS-mutated solid tumors.

(1R)-KRAS inhibitor-24 (compound 115c) is a pyridino-pyridine KRAS inhibitor with an IC50 of less than 100 nM for KRas G12V, KRas WT, and KRas G12R.

SOS1-IN-7 (compound 18-p1) is a potent SOS1 inhibitor with IC50 values of 20 nM for SOS1-G12D and 67 nM for SOS1-G12V.

SOS1-IN-6 (compound 33-P1) is a potent inhibitor of SOS1, exhibiting an IC50 of 14.9 nM on SOS1-G12D and 73.3 nM on SOS1-G12V.

SOS1-IN-8 is an inhibitor of SOS1 and acts on SOS1-G12D (IC50: 11.6 nM) and SOS1-G12V (IC50: 40.7 nM).

SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity ( EC 50 =106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS [1] .

Pan-KRAS-IN-6 (compound 12) is a potent pan-KRAS inhibitor, with IC50 values of 9.79 nM for Kras G12D and 6.03 nM for Kras G12V.

KRAS inhibitor-24 (compound 115c), a pyrido-pyridine class KRAS inhibitor, exhibits potent activity against KRas G12V, KRas WT, and KRas G12R, with IC50 values all below 100 nM.

K-Ras-IN-3 (compound 3) is an effective inhibitor of GDP-KRAS G12V, exhibiting an IC50 value of 0.371 nM. It has potential for use in cancer research.

KRAS inhibitor-26 (compound 194a) is an effective inhibitor of KRAS G12V (IC50: ≤100 nM), primarily utilized in cancer research.