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Results for "

oncogenic mutant

" in MedChemExpress (MCE) Product Catalog:

17

Inhibitors & Agonists

1

Peptides

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12408A
    6H05 TFA

    		Ras Cancer
    6H05 TFA is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
    6H05 TFA
  • HY-148439
    RMC-6236
    1 Publications Verification

    RAS-IN-2

    		 Ras PERK Cancer
    RMC-6236 is an orally active, non-covalent RAS (ON) inhibitor. RMC-6236 disrupts the interaction of wild-type or mutant RAS proteins with the RAS binding domain of BRAF, with EC50 values ranging from 28-220 nM for wild-type KRAS, NRAS, HRAS, and multiple oncogenic RAS variants. RMC-6236 inhibits pERK. RMC-6236 has anti-tumor activity against KRAS mutant tumors .
    RMC-6236
  • HY-136789
    Tuxobertinib
    1 Publications Verification

    BDTX-189

    		 EGFR Cancer
    Tuxobertinib (BDTX-189) is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. Tuxobertinib shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity .
    Tuxobertinib
  • HY-153386
    CPD-1224

    		Anaplastic lymphoma kinase (ALK) Cancer
    CPD-1224 is an orally effective ALK inhibitor, a derivative of an ALK inhibitor that connects to the cereblon ligand. CPD-1224 targets the EML4-ALK oncogenic fusion protein and degrades both ALK and the mutant forms L1196M/G1202R. CPD-1224 can slow down tumor growth .
    CPD-1224
  • HY-151287
    KRAS inhibitor-20

    		Ras Cancer
    KRAS inhibitor-20 is a small molecular inhibitor of KRas G12C, the oncogenic mutant. KRAS inhibitor-20 inhibits KRas G12C with the IC50 value <10 nM .
    KRAS inhibitor-20
  • HY-12408
    6H05

    		Ras Cancer
    6H05 is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
    6H05
  • HY-120885
    (+)-Oxanthromicin

    		Ras Cancer
    (+)-Oxanthromicin (Compound 1) mislocalizes the oncogenic mutant K-Ras from the plasma membrane of intact Madin-Darby canine kidney (MDCK) cells, and exhibits thereby antitumor efficacy .
    (+)-Oxanthromicin
  • HY-164482
    HG-6-63-01

    		RET Cancer
    HG-6-63-01 is a type II RET tyrosine kinase inhibitor (TKI). HG-6-63-01 also inhibits REarranged during Transfection (RET) kinase and signaling in human thyroid cancer cell lines carrying oncogenic RET alleles. HG-6-63-01 impairs phosphorylation and signalling of RET oncogenic mutants. HG-6-63-01 blunts proliferation of RET/C634R and RET/M918T-transformed fibroblasts and of RET mutant thyroid cancer cells, which is promising for research of cancers harboring oncogenic activation of RET .
    HG-6-63-01
  • HY-164467
    CCT070535

    		Wnt Cancer
    CCT070535 blocks TCF-dependent transcription at the TCF level, with GI50 values of 17.6 μM, 11.1 μM, 11.8 μM and 13.4 μM in HT29 (APC mutant), HCT116 (oncogenic β-catenin), SW480 (APC mutant) and SNU475 (Axin mutant) cells, respectively .
    CCT070535
  • HY-164488
    KT D606

    		PAK Cancer
    KT D606 is an inhibitor of the PAK kinase family, with an IC50 value of 4 μM. KT D606 selectively blocks the proliferation of cancer cells transformed by oncogenic RAS mutants and can be used for research on RAS/PAK1-induced cancers .
    KT D606
  • HY-P10436
    Braftide

    		Raf Cancer
    Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAF G469A with IC50 of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC50 is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence .
    Braftide
  • HY-122914
    KRAS inhibitor-3

    		Ras Cancer
    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 KRAS G12D, 0.74 μM for KRAS Q61H). KRAS inhibitor-3 also disrupts interaction of KRAS with Raf .
    KRAS inhibitor-3
  • HY-139590
    Zeteletinib

    BOS-172738; DS-5010

    		 RET PDGFR Cancer
    Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity .
    Zeteletinib
  • HY-107779
    BI-882370

    		Raf Cancer
    BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAF V600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases .
    BI-882370
  • HY-139590A
    Zeteletinib hemiadipate

    BOS-172738 hemiadipate; DS-5010 hemiadipate

    		 RET PDGFR Cancer
    Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib hemiadipate has potent antitumor activity .
    Zeteletinib hemiadipate
  • HY-150926
    G12Si-1

    		Ras Cancer
    G12Si-1 is a selective K-Ras(G12S) covalent inhibitor, which can inhibit oncogenic signaling of K-Ras(G12S). G12Si-1 shows good ability to covalently engage recombinant K-Ras(G12S) at the mutant serine residue. G12Si-1 can also affect nucleotide cycling of K-Ras by blocking Sos-catalyzed exchange and decreasing the rate of EDTA promoted exchange .
    G12Si-1
  • HY-157228
    ACBI3

    		PROTACs Ras Cancer
    ACBI3 (compound 7) is a PROTAC targeting KRAS. ACBI3 is composed of PROTAC target protein ligand pan-KRAS degrader 1 (HY-162960) (red part), E3 ligase ligand E3 ligase Ligand 43 (HY-401613) (blue part) and PROTAC Linker 1-Bromo-4-(ethynyloxy)butane (HY-169992) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 143 (HY-169995). ACBI3 achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models .
    ACBI3

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