Scientific Reviews
Product Guides
Blogs
Topics
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
98 Results for "
resistance mutation
" in MedChemExpress (MCE) Product Catalog:
Products (98)
98 Results for "resistance mutation" in MCE Product Catalog:
25
Target:
Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle .
14
14 Cited Publications
RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin (HY-10219) with MLN0128 (HY-13328, a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR. RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity .
9
Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
9
9 Cited Publications
Synonyms: HS-10296 mesylate
Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer .
9
9 Cited Publications
Synonyms: HS-10296 hydrochloride
Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer .
3
3 Cited Publications
Synonyms: BDTX-1535; EGFR-IN-76
Target:
Research Areas:
Silevertinib (BDTX-1535) is an irreversible, brain-penetrant, selective and orally active EGFR inhibitor with wild-type EGFR-sparing. Silevertinib targets key EGFR resistance mutations, including the kinase domain (C797S, L718Q, G724S, S768I), extracellular domain (EGFRvIII, A289X), and EGFR amplification. Silevertinib exerts anti-tumor activity with well tolerated in vivo. Silevertinib can be used for non-small cell lung cancer (NSCLC) and glioblastoma (GBM) research .
2
2 Cited Publications
Anguizole is an HCV NS4B inhibitor. Anguizole interacts with NS4B-AH2, inhibits AH2 lipid vesicle aggregation, disrupts NS4B dimerization/multimerization and impairs NS4B-NS5A interaction. Anguizole exhibits little host cell toxicity. Anguizole can be used for the research of HCV infection .
1
Lirafugratinib (RLY-4008) is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib covalently binds to Cys491. Lirafugratinib targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .
1
1 Cited Publications
Synonyms: RLY-4008 hydrochloride
Lirafugratinib (RLY-4008) hydrochloride is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib hydrochloride covalently binds to Cys491. Lirafugratinib hydrochloride targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .
1
Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity .
1
1 Cited Publications
Research Areas:
PDD00017272 is an inhibitor of poly(ADP-ribose) glycohydrolase (PARG) (EC50=4.8 nM) and an activator of PARP1/2. PDD00017272 inhibits its activity of hydrolyzing poly(ADP-ribose) (pADPr), resulting in the accumulation of pADPr on chromatin, interfering with DNA damage repair and replication processes, and inducing PARP1/2-dependent cytotoxicity. PDD00017272 can be used in cancer models with DNA repair defects (such as BRCA mutations) or resistance to PARP inhibitors. PDD00017272 has a PARG expression level-correlated inhibitory potency with EC50 of 9.2 nM (PARG cells), the tumor cells with lower PARG expression are more sensitive .
Synonyms: STP1002
Basroparib (STP1002) is a selective, orally active inhibitor of tankyrase (TNKS1/TNKS2) with IC50 of 29.94 nM and 3.68 nM for TNKS1 and TNKS2, respectively. Basroparib has an IC50 of >10 μM for PARP1. Basroparib binds to TNKS, stabilizes AXIN1/2 proteins, blocks Wnt/β-catenin signaling pathway, inhibits tumor cell proliferation and induces apoptosis, while reducing cancer stem cell properties. Basroparib can be used in colorectal cancer (CRC) studies with KRAS mutations (such as G12V/G12D) to overcome acquired resistance to MEK inhibitors. STP1002 has synergistic antitumor activity with MEK inhibitors .
Synonyms: NVL-520; NUV-520
Target:
Research Areas:
Zidesamtinib (NVL-520) is a potent, selective, orally active and brain-penetrant inhibitor of diverse ROS1 fusions and resistance mutations, with IC50s of 0.7 and 7.9 nM for wild-type ROS1 and ROS1 G2032R, respectively, and spares TRK inhibition. Zidesamtinib can be used for the research of cancer .
Cat. No.: HY-148811
CAS No.: 2403703-30-8
Synonyms: ICP-723
Target:
Research Areas:
Zurletrectinib is a brain-penetrant, orally active TRK inhibitor (TRKA IC50 = 0.81 nM; TRKB IC50 = 0.145 nM; TRKC IC50 = 0.184 nM). Zurletrectinib exhibits stronger activity as a consequence of its augmented binding affinity for TRK kinases. Zurletrectinib exhibits higher activity against most TRK inhibitor resistance mutations (13 out of 18 mutations). Zurletrectinib can be used for the study of glioma .
Cat. No.: HY-172262
Target:
Research Areas:
WEHI-3773 is a VDAC2 ligand and apoptosis modulator. WEHI-3773 directly binds to the β7-β10 region of VDAC2 and disrupts its interaction with BAX and BAK. WEHI-3773 regulates BAX-mediated apoptosis in BAK-deficient cells by modulating conformational activation of BAX, mitochondrial redistribution, and cytochrome c release. WEHI-3773 overcomes Venetoclax (HY-15531) resistance, resensitizes leukemia cells carrying BAX mutations to BH3 mimetics, and enables long-term clonogenic survival of BAK-deficient cells treated with BH3 mimetics. WEHI-3773 is applicable to research related to acute myeloid leukemia .
SJF-0628 is a PROTAC degrader of BRAF mutants, with a DC50 of 6.8 nM against BRAF V600E. SJF-0628 induces the ubiquitination and degradation of BRAF mutants in various cancer cell lines. SJF-0628 reduces pMEK and pErk levels. SJF-0628 exhibits antitumor activity. SJF-0628 can be used in research on colorectal cancer, melanoma, lung cancer, and triple-negative breast cancer .
Cat. No.: HY-19815
CAS No.: 1660963-42-7
Synonyms: CK-101; RX518
Olafertinib (CK-101) is an orally available, third generation and irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). Olafertinib selectively inhibits both EGFR-TKI-sensitizing and resistance mutations with minimal activity on wild-type EGFR. Olafertinib can be used in research for non-small cell lung cancer (NSCLC) with EGFR mutations and other advanced malignancies .
Cat. No.: HY-137849
CAS No.: 2171388-28-4
RK-582 is a tankyrase inhibitor, antitumor agent, and orally bioavailable growth inhibitor, with an IC50 of 36.1 nM against human tankyrase-1 and an IC50 of 39.2 nM against human tankyrase-2. In APC-mutated colorectal cancer cells, the sensitivity to RK-582 correlates with the level of active β-catenin, while drug resistance associates with PIK3CA mutation. RK-582 can be used for the research of colorectal cancer .
TNG260 is a selective, orally effective inhibitor of HDAC1 and CoREST complex, with a 10-fold selectivity for HDAC1 over HDAC3 and a 500-fold selectivity for CoREST complex over NuRD and Sin3 complex. TNG260 reshapes the tumor immune microenvironment, reduces immunosuppressive neutrophil infiltration, promotes effector T cell recruitment, and reverses anti-PD-1 resistance caused by STK11 deficiency by inhibiting the activity of the CoREST-HDAC1 complex. TNG260 induces durable tumor regression in combination with α-PD1 in MC38 tumor-bearing mice with STK11 mutations, and has lower toxicity to bone marrow cells than non-selective HDAC inhibitors .
Target:
Research Areas:
AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells .
-
-
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
