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KRASG12D inhibitor 14 is a potent KRASG12D inhibitor with a KD of 33 nM for binding to KRASG12D protein. KRASG12D inhibitor 14 decreases the active form of KRASG12D (KRASG12D-GTP) but not KRAS G13D .
RMC-9805 (KRASG12D inhibitor 18) is a KRASG12D inhibitor. RMC-9805 is orally active. RMC-9805 inhibits RAS signaling to induce apoptosis in KRASG12D mutant cancer cells .
KRASG12D inhibitor 3 TFA is a KRASG12D inhibitor with an IC50 of <500 nM. KRASG12D inhibitor 3 TFA has antitumor effects (WO2022002102A1; compound 146) . KRASG12D inhibitor 3 (TFA) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
KRASG12D inhibitor 3 is a KRASG12D inhibitor with an IC50 of <500 nM. KRASG12D inhibitor 3 has antitumor effects (WO2022002102A1; compound 146) . KRASG12D inhibitor 3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
KRASG12D inhibitor 22 (compound 6) is a inhibitor of KRAS mutation. KRASG12D inhibitor 22 has high activity (IC50＜100 nM), good selectivity and low toxicity.KRASG12D inhibitor 22 can be used in breast cancer research .
KRASG12D inhibitor 15 is a potent inhibitor of KRASG12D. KRASG12D inhibitor 15 has the potential for the research of various diseases or disorders, such as cancer or cancer metastasis (extracted from patent WO2022042630A1, compound 243) . KRASG12D inhibitor 15 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
KRASG12D inhibitor 16 is a KRASG12D inhibitor. KRASG12D inhibitor 16 has inhibitory activity against KRASG12D and KRASG12D mutation with IC50 value of 0.7 nM and 0.35 μM, respectively. KRASG12D inhibitor 16 can be used for the research of many malignant tumor, such as pancreatic ductal adenocarcinomas (PDAC), colon and rectal carcinomas (CRC), non-small cell lung carcinomas (NSCLC) .
KRASG12D modulator-1 (compound 6) is a potent KRASG12D modulator with IC50 values of 1-10 μM for NEA-G12D, PPI-G12D, and p ERK-AGS, respectively. KRASG12D modulator-1 can be used in research of cancer .
KRASG12D inhibitor 23 (compound 46-3) is a potent inhibitor of KRASG12D, with the IC50 of 0.007 μM. KRASG12D inhibitor 23 plays an important role in cancer research .
KRASG12D inhibitor 1 (example 243) is a KRASG12D inhibitor, with an IC50 of 0.8 nM for KRASG12D-mediated ERK phosphorylation . KRASG12D inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
KRASG12D inhibitor 11 is a potent inhibitor of KRASG12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRASG12D inhibitor 11 has the potential for the research of KRASG12D-mediated cancer (extracted from patent WO2021108683A1, compound 52) .
KRASG12D inhibitor 12 is a potent inhibitor of KRASG12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRASG12D inhibitor 12 has the potential for the research of KRASG12D-mediated cancer (extracted from patent WO2021108683A1, compound 134) .
KRASG12D inhibitor 9 is a potent inhibitor of KRASG12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRASG12D inhibitor 9 has the potential for the research of KRASG12D-mediated cancer (extracted from patent WO2021108683A1, compound 20) .
KRASG12D inhibitor 10 is a potent inhibitor of KRASG12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRASG12D inhibitor 10 has the potential for the research of KRASG12D-mediated cancer (extracted from patent WO2021108683A1, compound 34) .
KRASG12D inhibitor 13 is a potent inhibitor of KRASG12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRASG12D inhibitor 13 has the potential for the research of KRASG12D-mediated cancer (extracted from patent WO2021108683A1, compound 142) .
KRASG12D inhibitor 8 is a potent inhibitor of KRASG12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRASG12D inhibitor 8 has the potential for the research of KRASG12D-mediated cancer (extracted from patent WO2021107160A1, compound 2) .
KRASG12D inhibitor 25 (Compound 148) is an inhibitor for KRAS G12C and HSP90α with IC50 of < 0.1 μM and 0.1-1 μM, respectively. KRASG12D inhibitor 25 inhibits the proliferation of MIA PaCa-2 and NCI-H358 with EC50 of < 0.1 μM and 0.1-1 μM, respectively. KRASG12D inhibitor 25 degrades ERBB2 with a DC50 of 0.1-1 μM .
Setidegrasib (example 8) is a quinazoline-linked (4R)-4-hydroxy-L-prolinamide compound, inducing degradation of G12D-mutation KRAS protein. Setidegrasib is a PROTAC .
KRASG12D-IN-3 (compound Z1084) is an orally active KRASG12D inhibitor that inhibits the cell growth of AGS and AsPC-1 cells with IC50 values of 0.38 nM and 1.23 nM, respectively .
KRASG12D-IN-1 (compound 22) is a KRASG12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
KRASG12D-IN-2 (compound 28) is a KRASG12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
PROTAC KRASG12D degrader 1 is a potent, rapid, and selective degrader of protac KRASG12D with DC 50 of 38.06 nM. PROTAC KRASG12D degrader 1 showes significant antitumor efficacy .
PROTAC KRASG12D degrades SARS-CoV-2, 3-curd trypsin-like protease (3CLPro). Protac KRASG12D degrades SARS-CoV-2, 3-curd trypsin-like protease (3CLPRO). The PROTAC molecule is designed by partially coupling a GC-376-based dipeptidyl 3CLPro ligand with pomadomide via a piperazine-piperidine linker .
MRTX1133 is a noncovalent, potent, and selective KRASG12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRASG12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRASG12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRASG12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRASG12D mutations .
KRAS inhibitor-31 (compound 33) is a KRAS inhibitor, with KD (SPR) values of 0.019 nM, 0.019 nM and 0.096 nM for KRasG12D, KRas G12C and KRas G12V, respectively .
KRAS inhibitor-37 (compound 2) is a potent KRAS inhibitor with KDs of 0.004 nM, 0.041 nM, 0.019 nM and 0.144 nM for KRAS wild type, KRASG12D, KRAS G12C and KRAS G12V by SPR binding assay, respectively. KRAS inhibitor-37 inhibits cell proliferation with IC50s of <2 nM-14 nM for H358, SW620, PANC08.13 cells, respectively. KRAS inhibitor-37 has the potential for cancer research .
(R)-G12Di-7 is a covalent ligand for KRAS-G12D, which selectively labels K-Ras-G12D·GDP and K-Ras-G12D·GppNHp. (R)-G12Di-7 exhibits inhibitory activity against G12D mutated cancer cells .
TH-Z827 is a mutant selective KRAS(G12D) inhibitor with an IC50 of 2.4 μM. TH-Z827 does not bind KRAS(WT) or KRAS(G12C). TH-Z827 blocked the KRAS(G12D)-CRAF interaction with an IC50 value of 42 μM .
MRTX-EX185 is a potent inhibitor of GDP-loaded KRAS and KRAS(G12D), with an IC50 of 90 nM for KRAS(G12D). MRTX-EX185 also binds GDP-loaded HRAS . MRTX-EX185 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MRTX-EX185 formic is a potent inhibitor of GDP-loaded KRAS and KRAS(G12D), with an IC50 of 90 nM for KRAS(G12D). MRTX-EX185 formic also binds GDP-loaded HRAS . MRTX-EX185 (formic) is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Pan-RAS-IN-4 (compound 2) is a potent inhibitor of RAS, with the IC50 of ＜ 100 nM for KRASG12D. Pan-RAS-IN-4 plays an important rile in cancer research .
KRAS inhibitor-22 (compound FB9/6B9) is a potent inhibitor of K-Ras. KRAS inhibitor-22 targets to Kras 4B(G12D) and (G12C), which can be used for cancer research .
TH-Z835 is a mutant selective KRAS(G12D) inhibitor with an IC50 of 1.6 μM. TH-Z835 inhibits both mantGMPPNP/GPPNP exchange and GPPNP/mantGMPPNP exchange .
pan-KRAS-IN-7 (Compound 25) is an inhibitor for in human tumor mutated genes KRAS, which inhibits proliferation of KRAS mutated cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 of 0.35 and 0.51 nM, respectively .
pan-KRAS-IN-8 (Compound 38) is an inhibitor for in human tumor mutated genes KRAS, which inhibits proliferation of KRAS mutated cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 of 0.07 and 0.18 nM, respectively .
pan-KRAS-IN-9 (Compound 52) is an inhibitor for in human tumor mutated genes KRAS, which inhibits proliferation of KRAS mutated cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 of 0.24 and 0.30 nM, respectively .
pan-KRAS-IN-10 (Compound 58) is an inhibitor for in human tumor mutated genes KRAS, which inhibits proliferation of KRAS mutated cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 of 0.7 and 0.24 nM, respectively .
PROTAC K-Ras Degrader-3 (compound 40) is a PROTAC degrader of K-Ras with a DC50 of ≤ 1 nM against SW620 KRASG12D, and a GI50 of ≤ 10 nM against SW620 3D cell growth. PROTAC K-Ras Degrader-3 can be utilized in cancer research .
pan-KRAS-IN-2 (compound 6) is a pan inhibitor of with IC50s ≤10 nM for KRAS WT and mutants (G12D, G12C, G12V, G12S, G12A, Q61H), and ＞10 μM for KRAS G13D, respectively .
KRAS inhibitor-3 is an inhibitor of KRAS inhibitor. KRAS inhibitor-3 binds to WT and oncogenic KRAS mutants with high affinity (KD: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRASG12D, 0.74 μM for KRAS Q61H). KRAS inhibitor-3 also disrupts interaction of KRAS with Raf .
K-Ras-IN-1 is a small molecule K-Ras inhibitor. K-Ras-IN-1 binds to K-Ras (WT), K-Ras (G12D), K-Ras (G12V), and H-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure. K-Ras-IN-1 is promising for research of pancreatic, colon and lung cancer .
HRS-4642 is a selective KRAS(G12D) inhibitor (Kd=0.083 nM) with anti-cancer activity. HRS-4642 synergizes with Carfilzomib (HY-10455) and exhibits significant in vivo potency to reshape the tumor microenvironment into an immune-activating microenvironment.
KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRASG12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells .
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC50 values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12DKRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer .
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 (EC50=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 .
SIAIS562055 is a potent cereblon-based SOS1 PROTAC with a Kd of 95.9 nM. SIAIS562055 exhibits sustained degradation of SOS1 and inhibition of downstream ERK pathways. SIAIS562055 effectively blocked the binding of KRASG12C or KRASG12D to SOS1, with the IC50 values of 95.7 nM and 134.5 nM, respectively. SIAIS562055 exhibits potent anticancer activity. (Pink: SOS1 ligand (HY-168638); Black: linker (HY-W539874); Blue: E3 ligase ligand (HY-W076696)) .
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 .
Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
Rineterkib hydrochloride (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated?MTOR?mutants and the growth of rapamycin-resistant cancer cells.?BC-LI-0186 is a promising agent for lung cancer research .
Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
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 (EC50=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 .
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
HLA-A*1101as is a key MHCI molecule that presents viral and tumor-derived peptides that direct T cell immune responses against infected or transformed cells. It collaborates with B2M to showcase a diverse peptide library. HLA-A*1101 KRAS G12D Protein, Human (HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-A*1101 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and VVVGADGVGK peptide. HLA-A*1101 KRAS G12D Protein, Human (HEK293, His-Avi), has molecular weight of 51-60 kDa.
HLA-A*1101as is a key MHCI molecule that presents viral and tumor-derived peptides that direct T cell immune responses against infected or transformed cells. It collaborates with B2M to showcase a diverse peptide library. HLA-A*1101 KRAS G12D Tetramer Protein, Human (HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-A*1101 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and VVVGADGVGK peptide. HLA-A*1101 KRAS G12D Tetramer Protein, Human (HEK293, His-Avi), has molecular weight of 260-265 kDa.
HLA-A*1101as, a pivotal MHCI molecule, presents viral and tumor-derived peptides, guiding T cell immune responses against infected or transformed cells. Collaborating with B2M, it displays a diverse peptide repertoire. Both the presented peptide and MHCI contribute to antigen recognition specificity. HLA-A*1101 typically presents 8 to 13 amino acid intracellular peptides, binding different peptides with allele-specific motifs. It plays a crucial role in controlling infections, presenting immunodominant epitopes from HIV-1, EBV, HBV, and contributing to the immune response against SARS-CoV-2. HLA-A*1101 KRAS G12D Complex Protein, Human (Biotinylated, VVVGADGVGK, HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-A*1101 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and VVVGADGVGK peptide. HLA-A*1101 KRAS G12D Complex Protein, Human (Biotinylated, VVVGADGVGK, HEK293, His-Avi), has molecular weight of 51-60 kDa.
The HLA-C*0304 KRAS G12D Complex, a major histocompatibility complex class I (MHCI) molecule, plays crucial roles in reproduction and antiviral immunity. Teaming up with B2M, it presents self and viral peptides, acting as a dominant ligand for inhibitory and activating killer immunoglobulin receptors (KIRs) on NK cells. In allogeneic contexts, it facilitates trophoblast interactions with NK cells, crucial for placental development. During viral infections, HLA-C*0304 may disrupt KIR-mediated inhibition and promote infected cell lysis. In adaptive immunity, it presents viral peptides to CD8-positive T cells, contributing to antigen-specific T cell responses in chronic viral infections. HLA-C*0304's fine specificity for antigen recognition and its role in immune surveillance stem from its ability to recognize diverse peptides and specific MHC residues. HLA-C*0304 KRAS G12D Complex Protein, Human (Biotinylated, GADGVGKSAL, HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-C*0304 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and GADGVGKSAL peptide. HLA-C*0304 KRAS G12D Complex Protein, Human (Biotinylated, GADGVGKSAL, HEK293, His-Avi), has molecular weight of 55-65 kDa.
The HLA-C*0304 KRAS G12D complex is a major histocompatibility complex class I (MHCI) molecule that plays a crucial role in reproduction and antiviral immunity. It collaborates with B2M to present self- and viral peptides as primary ligands that inhibit and activate killer immunoglobulin receptors (KIRs) on NK cells. HLA-C*0304 KRAS G12D Complex Protein, Human (GADGVGKSAL, HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-C*0304 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and GADGVGKSAL peptide. HLA-C*0304 KRAS G12D Complex Protein, Human (GADGVGKSAL, HEK293, His-Avi), has molecular weight of 55-65 kDa.
The HLA-C*0304 KRAS G12D complex is a major histocompatibility complex class I (MHCI) molecule that plays a crucial role in reproduction and antiviral immunity. It collaborates with B2M to present self- and viral peptides as primary ligands that inhibit and activate killer immunoglobulin receptors (KIRs) on NK cells. HLA-C*0304 KRAS G12D Complex Tetramer Protein, Human (GADGVGKSAL, HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-C*0304 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and GADGVGKSAL peptide. HLA-C*0304 KRAS G12D Complex Tetramer Protein, Human (GADGVGKSAL, HEK293, His-Avi), has molecular weight of 260-265 kDa.
KRASG12D-IN-1 (compound 22) is a KRASG12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
KRASG12D-IN-2 (compound 28) is a KRASG12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
KRASG12D inhibitor 3 TFA is a KRASG12D inhibitor with an IC50 of <500 nM. KRASG12D inhibitor 3 TFA has antitumor effects (WO2022002102A1; compound 146) . KRASG12D inhibitor 3 (TFA) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
KRASG12D inhibitor 1 (example 243) is a KRASG12D inhibitor, with an IC50 of 0.8 nM for KRASG12D-mediated ERK phosphorylation . KRASG12D inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
KRASG12D-IN-1 (compound 22) is a KRASG12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
KRASG12D-IN-2 (compound 28) is a KRASG12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
MRTX1133 is a noncovalent, potent, and selective KRASG12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRASG12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRASG12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRASG12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRASG12D mutations .
KRASG12D inhibitor 3 is a KRASG12D inhibitor with an IC50 of <500 nM. KRASG12D inhibitor 3 has antitumor effects (WO2022002102A1; compound 146) . KRASG12D inhibitor 3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
KRASG12D inhibitor 15 is a potent inhibitor of KRASG12D. KRASG12D inhibitor 15 has the potential for the research of various diseases or disorders, such as cancer or cancer metastasis (extracted from patent WO2022042630A1, compound 243) . KRASG12D inhibitor 15 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
KRASG12D inhibitor 23 (compound 46-3) is a potent inhibitor of KRASG12D, with the IC50 of 0.007 μM. KRASG12D inhibitor 23 plays an important role in cancer research .
KRAS inhibitor-31 (compound 33) is a KRAS inhibitor, with KD (SPR) values of 0.019 nM, 0.019 nM and 0.096 nM for KRasG12D, KRas G12C and KRas G12V, respectively .
MRTX-EX185 is a potent inhibitor of GDP-loaded KRAS and KRAS(G12D), with an IC50 of 90 nM for KRAS(G12D). MRTX-EX185 also binds GDP-loaded HRAS . MRTX-EX185 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MRTX-EX185 formic is a potent inhibitor of GDP-loaded KRAS and KRAS(G12D), with an IC50 of 90 nM for KRAS(G12D). MRTX-EX185 formic also binds GDP-loaded HRAS . MRTX-EX185 (formic) is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
