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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
32 Results for "
H-358
" in MedChemExpress (MCE) Product Catalog:
Products (32)
32 Results for "H-358" in MCE Product Catalog:
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4 Cited Publications
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AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib (HY-10205) .
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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 .
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-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 .
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CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities .
BI-0474 is a potent KRAS G12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models .
Cat. No.: HY-144269
CAS No.: 2695506-82-0
SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC50s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAF wt, and bRAF V600E, respectively. SHR902275 shows cell growth inhibition with GI50s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively .
Cat. No.: HY-169311
CAS No.: 3058573-95-5
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, KRAS G12D, 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 .
Cat. No.: HY-159591
CAS No.: 3060515-08-1
YK-8S is a dual-targeted K-Ras (G12D/G12C) covalent inhibitor. YK-8S shows no significant binding to wild-type K-Ras and other mutants (G12R, G13D, Q61R/K). YK-8S exhibits anti-proliferative activity against H358 (G12C) and AGS (G12D) cells. YK-8S inhibits the phosphorylation of p-AKT/p-ERK in BaF3/G12D and G12C cells. YK-8S can be used for pancreatic cancer, colorectal cancer and other tumors with high incidence of G12D .
Cat. No.: HY-114436S
CAS No.: 2639608-44-7
Cat. No.: HY-144323
CAS No.: 2913177-53-2
YF135 is a KRAS G12C PROTAC degrader that mediates proteasomal degradation of KRAS G12C in a reversible manner. In KRAS G12C-mutant H358 and H23 lung cancer cells, the DC50 values of YF135 for KRAS degradation are 3.61 μM and 4.53 μM, respectively. YF135 attenuates the pERK signaling pathway in cancer cells. YF135 is applicable for lung cancer-related research .
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-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-142946
CAS No.: 2927439-07-2
KRAS G12C inhibitor 44 (compound 54) is a potent and orally active KRAS G12C inhibitor. KRAS G12C inhibitor 44 shows anti-proliferation activities with IC50s of 0.016, 0.028 µM in MIA PaCA-2, H358 cells, respectively. KRAS G12C inhibitor 44 shows antitumor effects in vivo .
Cat. No.: HY-115663
CAS No.: 902156-98-3
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C620-0696 is an inhibitor targeting the brom domain of BPTF, with a KD value of 35.5 μM. C620-0696 can exert cytotoxic effects on A549 and H358 cells, inhibiting the expression of c-Myc. C620-0696 inhibits cell migration and colony formation, and induces apoptosis and cell cycle arrest. C620-0696 can be used in the research of non-small cell lung cancer .
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-174088
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CDK4/6/BRD4-IN-2 (Compound PJ2) is a dual inhibitor of CDK4/6 and BRD4 with IC50 values for CDK4, CDK6, BRD4 (BD1), and BRD4 (BD2) of 168.75, 292.45, 23.17, and 3.12 nM respectively. CDK4/6/BRD4-IN-2 has a strong inhibitory effect on non-small cell lung cancer (NSCLC) cell lines. CDK4/6/BRD4-IN-2 induces cell cycle arrest, senescence and apoptosis through ROS-mediated DNA damage. CDK4/6/BRD4-IN-2 can also effectively inhibit the migration and invasion of NCI-H358 cells. CDK4/6-IN-2 can be used for the study of KRAS-mutated NSCLC .
Cat. No.: HY-172221
SOS1-IN-18 (Compound 8) is the inhibitor for Son of Sevenless 1 protein (SOS1) with a KD of 2.6 nM, and inhibits SOS1-KRAS G12C interaction with an IC50 of 3.4 nM. SOS1-IN-18 inhibits the phosphorylation of ERK in H358 with an IC50 of 31 nM, inhibits the proliferation of H358 with an IC50 of 5 nM .
Cat. No.: HY-115907
K20 is a potent and selective KRas G12C inhibitor with an IC50 of 1.16 µM. K20 shows anticancer activity in H358 cells (IC50= 0.78 µM). K20 decreases the levels of phosphorylated Erk and leads to cancer cell apoptosis. K20 suppresses NCI-H358 tumor growth with a TGI of 41% without causing obvious toxicity .
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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
