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MAPKKras
KRAS (Kirsten rat sarcoma virus) is a key member of the Ras protein family, belonging to the class of small GTPases that play a pivotal role in cellular signal transduction. It regulates cellular proliferation, differentiation, and survival by modulating pathways such as MAPK and PI3K. Mutations in the KRAS gene represent one of the most prevalent driver events in human tumours, occurring with high frequency particularly in pancreatic cancer, colorectal cancer, and non-small cell lung cancer. These mutations frequently result in the persistent activation of KRAS, triggering abnormal signalling pathways and promoting both tumour development and the emergence of drug resistance.
RMC-9805
T782122922732-54-3
RMC-9805 is a novel, mutant-selective, covalent and oral KRASG12D (ON) inhibitor. A stable and high affinity triple complex is formed between RMC-9805, KRASG12D, and cyclophilin A, which inhibits signal transduction downstream of KRASG12D (ON) by disrupting its interaction with downstream effectors. RMC-9805 can induce cell apoptosis and promote tumor regression in preclinical KRASG12D tumor models. With rich experience in compound synthesis, we can provide fast customized synthesis services for this product according to your research needs.
- $129
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MRTX1133
Cited
T93032621928-55-8In house
MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.
- $197
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CitedBI-2493
T720612937344-16-4In house
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.
- $629
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Adagrasib Cited
T83692326521-71-3
Adagrasib (MRTX849) is an orally active and selective covalent inhibitor of KRAS G12C. Adagrasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Adagrasib exhibits inhibitory activity against KRAS G12C mutant tumors.
- $59
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CitedDivarasib
T99722417987-45-0
Divarasib (GDC-6036) (GDC-6036) is an investigational, oral, high-potency and selective KRAS G12C inhibitor with an IC50 of < 0.01 μM. Divarasib irreversibly locks KRAS G12C oncoprotein in an inactive state and inhibits tumor cell growth. It is being investigated for use in solid tumors, including non-small cell lung and colorectal cancers and other types of cancer.
- $245
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BI-2865 Cited
T720622937327-93-8
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]
- $222
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CitedSotorasib Cited
T86842296729-00-3
Sotorasib (AMG-510) is an orally active and selective covalent inhibitor of KRAS G12C. Sotorasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Sotorasib exhibits inhibitory activity against KRAS G12C mutant tumors.
- $31
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Cited
T751312641998-63-0
RMC-6291 is an orally active, covalent inhibitor of KRAS G12C (ON) that forms a tri-complex within tumor cells between KRAS G12C (ON) and cyclophilin A (CypA), thereby preventing KRAS G12C (ON) from signaling via steric blockade of RAS effector binding and eliciting deep and durable suppression of RAS pathway activity in KRAS G12C tumor models [1].
- $162
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Glecirasib
T786512657613-87-9
Glecirasib (JAB-21822) is an orally active KRAS G12C inhibitor that selectively binds to and inhibits the activity of KRAS G12C mutants, thereby inhibiting KRAS G12C-dependent signaling. In animal models, KRAS G12C inhibitor 36 showed a favorable safety profile and potential to inhibit tumor growth.
- $113
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RMC-7977
T812632765082-12-8
RMC-7977 is a highly selective inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS with anticancer activity for the study of solid tumors with KRAS G12C mutations.
- $257
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T2040833040175-17-2
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.
- $337
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Lonafarnib
Cited
T6302193275-84-2
Lonafarnib (Sch66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B, and N-ras (IC50: 1.9/5.2/2.8 nM).
- $41
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CitedBI-3406 Cited
T129792230836-55-0
BI-3406 is an orally active, highly potent and selective between KRAS and Son of Sevenless 1 (SOS1) interaction inhibitor(IC50 : 6 nM),with anticancer activity.
- $67
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CitedT861672543673-19-2
DCC-3116 is an orally active, selective and potent ULK1/2 inhibitor with anticancer activity.DCC-3116 inhibits autophagy and can be used in cancer research.
- $115
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ACBI3
T855472938169-76-5
ACBI3 is a selective pan-KRAS degrader with anticancer activity that degrades oncogenic KRAS. ACBI3 inhibits the growth of most cancer cell lines driven by KRAS mutations.
- $272
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Paluratide
T796732676177-63-0
Paluratide (LUNA18) is a reversible cyclic peptide KRAS inhibitor with the advantages of oral availability and cell permeability for the treatment of kras-mutant cancers, which inhibits cancer cell proliferation by phosphorylating ERK and AKT, and also inhibits the interaction of RAS with guanine nucleotide exchange factors (GEFs).
- $1,180
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BI-2852 Cited
T105332375482-51-0In house
BI-2852 is a KRAS inhibitor targeting the switch I/II pocket (SI/II-pocket) with nanomolar affinity, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
- $118
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CitedK-Ras G12C-IN-4
T117382376328-55-9
K-Ras G12C-IN-4, is a potent Covalent Inhibitor of KRASG12C..
- $68
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GNE-9815
T95852729996-45-4
GNE-9815 (3-(2-cyanopropan-2-yl)-N-[2-fluoro-4-methyl-5-(7-methyl-8-oxo-7,8-dihydropyrido[2,3-d]pyridazin-3-yl)phenyl]benzamide) is a high kinase-selective inhibitor of RAF and targets KRAS-mutant cancers through combination therapy.
- $58
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KRAS G12C inhibitor 19
T402862649788-46-3
KRAS G12C inhibitor 19 is a potent KRAS G12C inhibitor that demonstrates anti-tumor activity in cellular assays and inhibits tumor growth [1].
- $83
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AMG-47a
T7123882663-88-9
AMG-47a is a potent inhibitor of Lck and T cell proliferation. AMG-47a could promote the degradation of the KRAS oncoprotein. AMG-47a selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells.
- $38
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Opnurasib
T402922653994-08-0
Opnurasib (JDQ-443) is an orally available and selective and potent covalent KRAS G12C inhibitor with antitumor activity for the study of advanced non-small cell lung cancer.
- $107
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Merodantoin
T33296143413-73-4In house
Merodantoin is an apoptosis inducer and triggers cell apoptosis associated with ROS-dependent autophagy. Merodantoin targets cancer cells expressing KRAS mutations involved in Akt-dependent ROS production.
- $70
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