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Results for "

mutation

" in TargetMol Product Catalog
  • Inhibitors & Agonists
    183
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Sotorasib
AMG-510
T86842296729-00-3
Sotorasib (AMG-510) is an orally active and selective covalent inhibitor of KRAS G12C. Sotorasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Sotorasib exhibits inhibitory activity against KRAS G12C mutant tumors.
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Leptomycin B
LMB, CI 940
T1573587081-35-4
Leptomycin B (LMB) is a potent inhibitor of the nuclear export of proteins and is a potent antifungal antibiotic blocking the eukaryotic cell cycle. Leptomycin B inactivates CRM1 exportin 1 by covalent modification at a cysteine residue.
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KRAS G12D mutation regulator 4
T778042621927-57-7
KRAS G12D mutation regulator 4 can be used in studies about Ras.
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8-10 weeks
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[Arg6]-β-Amyloid (1-42), england mutation
T83508
[Arg6]-β-Amyloid (1-42), England mutation, is a biologically active peptide linked to autosomal dominant Alzheimer's Disease in various kindreds. The English (H6R) mutation disrupts H6 interactions due to alterations in the beta-amyloid precursor gene.
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[Asn23]-beta-Amyloid (1-42), iowa mutation
T83506
[Asn23]-beta-Amyloid (1-42), Iowa mutation, is a biologically active peptide with increased aggregation propensity and fibril toxicity. This mutation involves the substitution of Aspartic acid (Asp) at position 23 with Asparagine (Asn), contributing to autosomal dominant Alzheimer's Disease and associated with severe cerebral amyloid beta-protein angiopathy (CAA) due to a missense alteration at position 694 of the amyloid precursor protein (APP) gene.
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[Asn23] β-Amyloid (1-40), Iowa mutation
T83507374796-72-2
[Asn23] β-Amyloid (1-40), Iowa mutation, is a biologically active peptide linked to autosomal dominant Alzheimer's Disease in multiple families. This involves the substitution of Asp 23 with Asn, causing severe cerebral amyloid beta-protein angiopathy (CAA). Individuals with this mutation exhibit a missense alteration in the APP gene at position 694, resulting in the mutated β-amyloid peptide aggregating more quickly and forming toxic fibrils.
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[Arg6]-β-Amyloid (1-40), england mutation
T835091802084-26-9
β-Amyloid (1-40), England mutation, is a biologically active peptide with a histidine (His) to arginine (Arg) substitution at position 6, known to enhance oligomerization kinetics that serve as fibril seeds and increase neurotoxicity in cultured neurons. This alteration is one of several mutations in the beta-amyloid precursor gene implicated in autosomal dominant Alzheimer's Disease across multiple kindreds.
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Gefitinib
ZD1839
T1181184475-35-2
Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.
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Quizartinib
AC220
T2066950769-58-1
Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases.
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Osimertinib
Mereletinib, AZD-9291
T24901421373-65-0
Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.
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gilteritinib
ASP2215
T44091254053-43-4
Gilteritinib (ASP2215) is a potent inhibitor of FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preclinical studies, gilteritinib demonstrated strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 clinical trials for acute myeloid leukemia.
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Bamocaftor
VX-659
T302932204245-48-5In house
Bamocaftor is a CFTR channel (DeltaF508-CFTR mutation) corrector for CF transmembrane conductance regulators designed to restore F508del-CFTR protein function. Combined use of tezacaftor and VX-561 for the treatment of cystic fibrosis patients with F508del MF.
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6-8weeks
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AGI-14100
AGI 14100
T250061448346-43-7In house
AGI-14100 is a novel and orally available mIDH1 inhibitor.AGI-14100 is used for the treatment of primary human myeloid leukemia.
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6-8weeks
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p53 Activator 7
T727712849340-59-4In house
p53 Activator 7 is a highly potent and cell-permeable activator of the p53 mutation Y220C (MDM-2 p53), which induces apoptosis.
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7-10 days
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N6-Allyladenosine
N-Allyladenosine, a6A, N Allyladenosine, N6-allyl adenosine
T3356315763-12-9In house
N6-Allyladenosine (N Allyladenosine), a novel small molecule for RNA tagging identified by mutation assays, is a nucleoside analogue with antimicrobial and anticancer activity that shows cytotoxicity against mammalian tumor cells and can be used in the study of breast cancer.
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6-8 weeks
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IDH2R140Q-IN-2
T797452749568-16-7In house
IDH2R140Q-IN-2 is an orally active and potent IDH2R140Q inhibitor with an IC50 of 29 nM.IDH2R140Q-IN-2 possesses potential antitumour activity, reducing D2HG production in TF-1 cell lines carrying the IDH2R140Q mutation (IC50 of 10 nM) and inhibiting tumour tissue D2HG levels.IDH2R140Q-IN-2 is suitable for the study of acute myeloid leukaemia (AML).
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6-8weeks
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NCGC00092410
ML008
T40544442898-34-2In house
NCGC00092410 (ML008) is a glucocerebrosidase (GC) inhibitor with IC50 value of 31 nM. It can be used for the study of Gaucher disease caused by mutation of glucocerebrase gene.
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Lopinavir
ABT-378
T1623192725-17-0
Lopinavir (ABT-378) is a peptidomimetic HIV protease inhibitor effective against HIV protease with the Val 82 mutation. It is less affected by serum protein binding compared to the structurally related drug ritonavir.
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Osimertinib mesylate
Mereletinib mesylate, AZD-9291 mesylate
T36341421373-66-1
Osimertinib mesylate (AZD-9291 mesylate) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib mesylate has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.
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o-Phenanthroline
1,10-Phenanthroline
T598366-71-7
o-Phenanthroline (1,10-Phenanthroline) , a metal chelator, prevents the induction of chromosomal aberrations in streptozotocin-treated cells.o-Phenanthroline protects mammalian cells from hydrogen peroxide-induced gene mutation and morphological transformation.
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Vemurafenib
RO5185426, RG7204, PLX4032
T2382918504-65-1
Vemurafenib (RG7204) is a B-RAF inhibitor that inhibits RAFV600E and c-RAF-1 (IC50=31 48 nM) selectively and potently. Vemurafenib exhibits antitumor activity and is used for the treatment of BRAF V600E mutation-positive melanoma.
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N-Acetyl-L-glutamic acid
N-Acetylglutamic acid, Ac-L-Glu-OH
T52671188-37-0
N-Acetyl-L-glutamic acid (Ac-L-Glu-OH) (NAcGlu) is an acetylated amino acid. NAcGlu is biosynthesized from glutamic acid and acetyl-CoA by the enzyme N-acetyl glutamate synthase (NAGS). NAcGlu activates carbamoyl phosphate synthetase in the urea cycle. A deficiency in N-acetyl glutamate synthase or a genetic mutation in the gene coding for the enzyme will lead to urea cycle failure in which ammonia is not converted to urea, but rather accumulated in the blood leading to the condition called Type I hyperammonemia.
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Lorlatinib
PF-6463922, PF-06463922, Loratinib
T30611454846-35-5
Lorlatinib (PF-6463922) is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.
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Erlotinib
R1415, OSI-744, NSC 718781, CP358774
T0373183321-74-6
Erlotinib (NSC-718781) is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.
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