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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
18 Results for "
KRAS mutant xenograft models
" in MedChemExpress (MCE) Product Catalog:
Products (18)
18 Results for "KRAS mutant xenograft models" in MCE Product Catalog:
ACBI3 (compound 7), a chemical probe, is a PROTAC targeting KRAS. ACBI3 achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models .
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MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12 .
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-W998345
SMART1 is a highly specific and CRBN-dependent PROTAC that can effectively degrade Smurf1. SMART1 can block the PDK1-Akt signaling pathway in KRAS mutant colorectal cancer. SMART1 can inhibit tumor growth in KRAS mutant colorectal cancer (CRC) xenograft models .
Cat. No.: HY-P991571
Synonyms: GC-1118A
Cat. No.: HY-175326
CAS No.: 2767633-04-3
SOS1-IN-21 is an orally active inhibitor of son of Sevenless 1 (SOS1) with an IC50 of 15 nM. SOS1 is a guanine nucleotide exchange factor (GEF) that activates KRAS by facilitating the exchange of GDP for GTP. SOS1-IN-21 exhibits potent antiproliferative activity, with IC50 values of 16 nM in NCI-H358 and 17 nM in Mia Paca-2 cell proliferation assays. SOS1-IN-21 exhibits significant antitumor activity in the Mia Paca-2 xenograft model. SOS1-IN-21 can be used for the study of KRAS mutant tumors, such as pancreatic cancer .
Cat. No.: HY-183365
SL43 is an orally active and potent SOS1 inhibitor with a Kd of 0.16 μM. SL43 disrupts SOS1-KRAS interaction, inhibits SOS1-mediated nucleotide exchange on KRAS mutants, and suppresses RAS-MAPK signaling. SL43 exerts antiproliferative activity against KRAS-mutant cancer cells, induces early apoptosis and G1 phase cell cycle arrest, and reduces phosphorylated MEK and ERK levels. SL43 suppresses tumor growth in a colorectal cancer xenograft model .
Cat. No.: HY-161173
CAS No.: 2836273-61-9
PROTAC SOS1 degrader-5 is a potent SOS1 PROTAC degrader with a DC50 value of 13 nM. PROTAC SOS1 degrader-5 induces CRBN-dependent ubiquitination and degradation of SOS1 protein, inhibits the proliferation of KRAS G12C-mutated cancer cells, and suppresses tumor growth in xenograft models. PROTAC SOS1 degrader-5 can be used in studies related to KRAS G12C-mutated non-small cell lung cancer .
Cat. No.: HY-186087
CAS No.: 3058972-05-4
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RM-046 is an orally active, selective ternary complex inhibitor of KRAS Q61H (active form). RM-046 forms a ternary complex with cyclophilin A, binds to active KRAS Q61H in a non-covalent manner, blocks effector binding via steric hindrance and inhibits downstream signal transduction. RM-046 inhibits ERK phosphorylation and cancer cell proliferation, and induces sustained RAS pathway signal inhibition, anti-tumor activity and tumor regression in preclinical xenograft models. RM-046 can be used for the research of KRAS Q61H mutant cancers .
Cat. No.: HY-186086
CAS No.: 2953276-07-6
RM-041 is a selective, orally active KRAS G13C (ON) inhibitor that forms a covalent complex with KRAS G13C (ON) and Cyclophilin A. RM-041 blocks the binding of RAS effector proteins via steric hindrance, and then covalently binds to Cys-13 to form an irreversible inhibitory complex, thereby inhibiting the proliferation of KRAS G13C mutant cancer cells. RM-041 induces regression of KRAS G13C tumors in cellular and xenograft tumor models. RM-041 exerts a synergistic effect when combined with upstream node inhibitors (such as SHP2 inhibitors). RM-041 can be used for the research of non-small cell lung cancer .
Cat. No.: HY-175870S
CAS No.: 3024881-00-0
Eras-4001-d6 is a deuterated form of Eras-4001 (HY-175870). 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-180200
CAS No.: 3032602-44-8
RNK08954 is an orally active KRASG12D inhibitor with a Kd of 0.0395 nM. RNK08954 selectively binds the inactive GDP-bound KRASG12D form, suppresses downstream KRAS-mediated signaling pathways p-ERK1/2 experssion. RNK08954 inhibits KRASG12D-mutant cell proliferation, induces G0-G1 cell cycle arrest, and inhibits tumor growth in mouse xenograft models. RNK08954 can be used for the research of non-small cell lung cancer, pancreatic ductal adenocarcinoma .
Cat. No.: HY-189278
KRAS-IN-64 is a KRAS inhibitor that inhibits KRAS translation by binding to and stabilizing the G-quadruplex in the 5'-UTR of KRAS mRNA, exhibits antiproliferative activity in KRAS-mutant cancer cells, and induces cell cycle arrest, non-apoptotic cell death, and PARP cleavage-mediated apoptosis (apoptosis). KRAS-IN-64 can be used for research on pancreatic cancer .
Cat. No.: HY-189222
CAS No.: 3118096-98-0
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RP04340 is an orally active, selective pan-KRAS PROTAC degrader. RP04340 hijacks the CRBN E3 ligase and the cellular proteasome system to degrade KRAS, without degrading HRAS, NRAS, or common CRBN neosubstrates. RP04340 inhibits KRAS downstream signaling pathways, including pERK and DUSP6. RP04340 exhibits anticancer activity in various KRAS-mutant cancers. RP04340 can be used to study kras-driven cancers, including pancreatic ductal adenocarcinoma, colorectal cancer, and lung adenocarcinoma .
Cat. No.: HY-183741
CAS No.: 3080226-63-4
VVD-844 is an orally active covalent inhibitor of PI3Kα, which inhibits Pl3Kα/p110α interaction with an IC50 of 4 nM. VVD-844 covalently binds to Cys 242 in the RAS binding domain of p110α, blocking RAS-p110α interaction and inhibiting PI3Kα activity. VVD-844 inhibits PI3Kα signaling activation in HER2-overexpressing cells via a RAS-independent mechanism. VVD-844 suppresses tumor growth in mouse. VVD-844 can be used for the research of cancers .
Cat. No.: HY-186283
CAS No.: 2719667-13-5
GNE-0749 is an orally active pan-RAF inhibitor with a Ki value of 0.061 nM against CRAF. GNE-0749 inhibits RAF dimer signaling via a DFG-out/αC-helix-in binding mode, prevents paradoxical activation of the MAPK pathway, and suppresses downstream MEK/ERK/RSK signal transduction. GNE-0749 can be used in studies related to KRAS G12C mutation-driven cancers .
Cat. No.: HY-186321
CAS No.: 501124-40-9
Synonyms: KF25706
Radicicol 6-oxime (KF25706) is an Hsp90 inhibitor with an EC50 of 5.5 nM against human Hsp90. Radicicol 6-oxime binds to Hsp90 and disrupts its chaperone function, leading to destabilization and depletion of Hsp90-associated signaling molecules. Radicicol 6-oxime depletes Hsp90-associated signaling proteins such as Raf-1, v-src, p185erbB2, Cdk4, and mutant p53, thereby inhibiting K-ras and v-src signaling pathways. Radicicol 6-oxime exhibits antiproliferative activity against various tumor cells. Radicicol 6-oxime inhibits tumor growth in mouse tumor xenograft models. Radicicol 6-oxime can be used for research on breast cancer, colon cancer, and vulvar epidermoid carcinoma .
Cat. No.: HY-184010
CAS No.: 3101973-42-3
BRSD-143 is an orally active KRAS G12D inhibitor, with a Kd value of 0.003 nM for KRAS G12D and 0.024 nM for KRAS G12V. BRSD-143 inhibits the activity of phosphorylated ERK in KRAS-mutated cells. BRSD-143 induces tumor regression in ovarian cancer xenograft mouse models. BRSD-143 can be used for the research of KRAS-mutated cancers .
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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
