mutants — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T9072	Tuxobertinib	BDTX-189	EGFR , HER , BTK , RIP kinase
	Tuxobertinib (BDTX-189) is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations(KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively). BDTX-189 exhibits anticancer activ...		EGFR , HER , BTK , RIP kinase
TQ0092	Naquotinib	ASP8273	EGFR
	Naquotinib (ASP8273) (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; (IC50s: 8-33 nM and 230 nM toward EGFR mutants and EGFR.		EGFR
T72062	BI-2865		Ras
	BI-2865 is a non-covalent pan-KRAS inhibitor.BI-2865 binds to KRAS WT, G12C, G12D, G12V, and G13D mutants with KD values of 6.9, 4.5, 32, 26, and 4.3 nM, respectively.BI-2865 showed antiproliferative activity in BaF3 cel...		Ras
T31014	Corrector C4	Corr 4a,Corrector C-4,Corr4a,Corrector C 4,Corr-4a	Others
	Corrector C4, a corrector commonly used to study cystic fibrosis mutants, works by alleviating the interaction between CFTR transmembrane domain mutants and protein homeostasis.		Others
T11761	Tarlox-TKI	Kinase inhibitor-1	EGFR
	Tarlox-TKI (Kinase inhibitor-1) is a pan-ErbB inhibitor, the active ingredient of Tarloxotinib, with antitumor activity.Tarlox-TKI inhibits NRG1 and suppresses HER2 mutants.		EGFR
T22592	ATPγS tetralithium salt	ATP-gamma-S tetralithium salt	PERK
	ATPγS tetralithium salt is a substrate for nucleotide hydrolysis and RNA unraveling activity of the eukaryotic translation initiation factor eIF4A, associated with p97 mutants and prions.		PERK
T24943	VPC-14228	VPC 14228,VPC14228	Androgen Receptor
	VPC-14228 is a specific AR-DBD inhibitor that acts by inhibiting both Y594A and Q592A mutants.		Androgen Receptor
T2104	AGI-5198	IDH-C35	Dehydrogenase , Isocitrate Dehydrogenase (IDH)
	AGI-5198 (IDH-C35) is a highly effective and specific inhibitor of IDH1 R132H/R132C mutants (IC50: 0.07/0.16 μM).		Dehydrogenase , Isocitrate Dehydrogenase (IDH)
T6824	EAI045		EGFR
	EAI045, an allosteric inhibitor, targets towards drug-resistant EGFR mutants but avoids the wild-type receptor.		EGFR
T16516	PG01	Phenylglycine-01	CFTR
	PG01 is a potent CFTR Cl-channel potentiator, effective against ΔF508 (Ka 0.3 μM), and also against E193K, G970R and G551D (CFTR mutants), with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively.PG01 increases ΔF508...		CFTR
T2147	Nilotinib monohydrochloride monohydrate	Nilotinib (monohydrochloride monohydrate),AMN107 (monohydrochloride monohydrate)	Bcr-Abl , Autophagy
	Nilotinib monohydrochloride monohydrate (Nilotinib (monohydrochloride monohydrate)) is significantly potent BCR-ABL against, is a second generation tyrosine kinase inhibitor (TKI), and is active against many BCR-ABL muta...		Bcr-Abl , Autophagy
T7861	Flumatinib mesylate	HHGV678 mesylate	Bcr-Abl , PDGFR , c-Kit
	Flumatinib mesylate (HHGV678 mesylate) is a selective inhibitor of c-Abl, PDGFRβ and c-Kit, effectively overcomes drug resistance of certain KIT mutants.		Bcr-Abl , PDGFR , c-Kit
T5084	Xanthosine dihydrate		Others , Endogenous Metabolite
	Xanthosine is produced by guanine-free mutants of bacteria e.g. Bacillus subtilis, Aerobacter aerogenes. Xanthosine monophosphate is an intermediate in purine metabolism, formed from IMP, and forming GMP.		Others , Endogenous Metabolite
T2287	PIK-75 hydrochloride	PIK-75 HCl,PIK-75	Apoptosis , DNA-PK , PI3K
	PIK-75 hydrochloride (PIK-75 HCl) is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM in cell-free assays.		Apoptosis , DNA-PK , PI3K
T6198	Dolutegravir	S/GSK1349572,GSK1349572	HIV Protease
	Dolutegravir (GSK1349572) (IC50=2.7 nM), a two-metal-binding HIV integrase inhibitor, exhibits medium activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.		HIV Protease
TQ0277	Pralsetinib	Blu667	c-RET
	Pralsetinib (Blu667) (BLU-667) is a highly potent, selective RET inhibitor (IC50s: 0.4, 0.3, 0.4, 0.4, and 0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion).		c-RET
T2620	G-749	G749	Apoptosis , FLT , c-RET , TAM Receptor , Aurora Kinase
	G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants.		Apoptosis , FLT , c-RET , TAM Receptor , Aurora Kinase
T2329	Dolutegravir sodium	GSK1349572,GSK-1349572A	HIV Protease
	Dolutegravir sodium (GSK-1349572A) salt(DTG; GSK1349572) is an HIV integrase inhibitor(IC50: 2.7 nM), modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.		HIV Protease
T22324	Ensartinib hydrochloride	Ensartinib dihydrochloride,X-396 dihydrochloride	Others , Trk receptor , c-Met/HGFR , ALK
	Ensartinib hydrochloride (X-396 dihydrochloride) is a potent new-generation ALK inhibitor with high activity against CNS metastases and a broad range of known crizotinib-resistant ALK mutations. It potently inhibits both...		Others , Trk receptor , c-Met/HGFR , ALK
T11438	GNE-1858		Others , MAPK
	GNE-1858 is an ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor (IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA).		Others , MAPK