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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
173 Results for "
K-Ras mutant
" in MedChemExpress (MCE) Product Catalog:
Products (173)
173 Results for "K-Ras mutant" in MCE Product Catalog:
Cat. No.: HY-154959A
Purity: 98.90%
(9R,12aR)-AZD4747 is a diastereomer of AZD4747 (HY-154959). AZD4747 is a selective mutant GTPase KRAS G12C inhibitor with blood-brain barrier permeability. AZD4747 has the potential to study cancer .
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(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.
Cat. No.: HY-175419
Synonyms: trans bis-Isatoic anhydride
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TBIA (trans bis-isatoic anhydride) is a covalent RNA crosslinker. TBIA selectively induces RNA tertiary interactions (e.g., multi-helix junctions, loop-helix packing). TBIA is promising for research of RNA higher-order structure and disease-associated RNAs (e.g., KRAS-mutant RNAs) .
Cat. No.: HY-161450
LHF418 is a SOS1 PROTAC degrader that induces the degradation of the target protein SOS1 by recruiting cereblon. LHF418 promotes the formation of the SOS1-PROTAC-CRBN ternary complex and induces SOS1 degradation in a cereblon- and proteasome-dependent manner. LHF418 inhibits EGF-induced ERK1/2 phosphorylation and the clonogenic growth of KRAS-mutant cancer cells. LHF418 can be used in studies related to SOS1-targeted protein degradation and KRAS-driven tumors .
Cat. No.: HY-168012
CAS No.: 3054023-07-0
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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-173250
YN14-H is a potent mutant KRAS G12C PROTAC degrader. The DC50 values of YN14-H in NCI-H358 and MIA PaCa-2 cells are 28.9 nM and 18.1 nM, respectively, with corresponding IC50 values of 42 nM and 21 nM. YN14-H degrades KRAS G12C in a ubiquitin-proteasome system-dependent manner, thereby significantly inducing apoptosis and inhibiting cell migration. YN14-H can be used for targeting tumors with KRAS G12C mutations (such as non-small cell lung cancer, pancreatic cancer, etc.) .
Cat. No.: HY-175575
CAS No.: 3027979-08-1
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SOS1 ligand-2 is a SOS1 ligand that can be used for PROTAC synthesis. SOS1 ligand-2 serves as the target protein ligand for PROTAC SOS1 degrader-4 (HY-153674). SOS1 ligand-2 is applicable to the research of KRAS-mutant cancers .
Cat. No.: HY-156498R
CAS No.: 2765082-12-8
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RMC-7977 (Standard) is the analytical standard of RMC-7977 (HY-156498). This product is intended for research and analytical applications. RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS G12C cancer models, and demonstrates good tolerability across various RAS cancer models .
Cat. No.: HY-160023
CAS No.: 2914919-85-8
Synonyms: D3S-001
Elisrasib (D3S-001) is an orally active and selective inhibitor for KRAS. Elisrasib inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2. D3S-001 also inhibits the phosphorylation of cellular ERK1/2. Elisrasib exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .
Cat. No.: HY-175870
CAS No.: 3024878-19-8
Eras-4001 is a potent, orally active pan-KRAS inhibitor with Kd values of 110, 13 and 39 pM against wild-type, G12D and G12V mutant KRAS, respectively, and exhibits selectivity toward wild-type HRAS and NRAS. Eras-4001 inhibits ERK1/2 phosphorylation and cell viability in cancer cells. Eras-4001 induces tumor growth inhibition and regression in subcutaneous xenograft models. Eras-4001 can be used in research on non-small cell lung cancer, ovarian cancer, etc.
Cat. No.: HY-149607
CAS No.: 2802453-88-7
SHP2-IN-22 is SHP2 allosteric inhibitor with an IC50 value of 17.7 nM. SHP2-IN-22 inhibits the proliferation, migration, and invasion of MIA PaCa-2 pancreatic cancer cells. SHP2-IN-22 can be used for Kirsten rat sarcoma viral oncogene (KRAS) mutant cancer research .
Cat. No.: HY-153674
PROTAC SOS1 degrader-4 (Compound 10) is a PROTAC degrader that targets the SOS1 protein for degradation by recruiting cereblon. It degrades SOS1 in NCI-H358, A-427, SW-620, and DLD-1 cells and inhibits the proliferation of various KRAS-mutant tumor cells, making it a useful tool for cancer research .
Cat. No.: HY-173405
CAS No.: 3055319-82-6
VVD-699 is a covalent blocker of the RAS-p110α interaction with oral activity. VVD-699 inhibits activation of PI3Kα (IC50: 104 nM in H358 cells) . VVD-699 inhibits phosphorylated AKT. VVD-699 can be used for the research of KRAS mutant/amplified cancer .
Cat. No.: HY-P991571
Synonyms: GC-1118A
Cat. No.: HY-184902
CAS No.: 3110809-62-3
FAK-IN-32 is an orally active, selective and highly potent FAK inhibitor (IC50 = 10.87 nM). FAK-IN-32 can induce cell cycle arrest at the G2/M phase, inhibit FAK-AKT signaling pathway activity, and promote apoptosis to some extent. FAK-IN-32 can be used for research on KRAS-mutant colorectal cancer .
GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits Ki values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers .
Cat. No.: HY-157458
CAS No.: 3054112-59-0
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PDEδ autophagic degrader 1 (compound 12c), an autophagosome-tethering compound (ATTEC). is a potent PDEδ autophagic degrader. PDEδ autophagic degrader 1 reduces the PDEδ protein level through lysosome-mediated autophagy without affecting the PDEδ mRNA expression. PDEδ autophagic degrader 1 suppresses the growth in KRAS mutant pancreatic cancer cells .
Cat. No.: HY-162281
CAS No.: 3032282-51-9
PROTAC SOS1 degrader-6 is a selective SOS1 PROTAC degrader with a DC50 of 43-130 nM. PROTAC SOS1 degrader-6 induces ubiquitination and degradation of SOS1 via the ubiquitin-proteasome system by recruiting the E3 ligase VHL. PROTAC SOS1 degrader-6 reduces the levels of phosphorylated MEK and ERK. PROTAC SOS1 degrader-6 exerts antiproliferative effects in KRAS-driven cancer cells. PROTAC SOS1 degrader-6 can be used in research related to KRAS G12C-mutant cancers and chronic myeloid leukemia .
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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
