mutant-selective — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T8485	THIQ		Melanocortin Receptor
	THIQ is a selective melanocortin-4 receptor (MC4R) agonist (hMC4R and rMC4R with IC50 of 1.2 nM and 0.6 nM , respectively).		Melanocortin Receptor
T7414	ARS-853		Apoptosis , Raf , Ras
	ARS-853 is an inhibitor of K-RASG12C(IC50 : 2.5 μM), a mutant form of K-RAS that accumulates in the active GTP-bound state in certain cancer cells		Apoptosis , Raf , Ras
T16143	MRTX-1257		Ras
	MRTX-1257 is a selective, irreversible, and covalent inhibitor of KRAS G12C. It has an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells. MRTX1257 demonstrated 31% bioavailability in the mouse, with fre...		Ras
T8369	Adagrasib	MRTX849	Ras
	Adagrasib (MRTX849) is an orally active and selective covalent inhibitor of KRAS G12C. Adagrasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Adagrasib ...		Ras
T60076	Oritinib	SH-1028	EGFR
	Oritinib (SH-1028) is an inhibitor of EGFR with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM for EGFR (wt), EGFR (L858R), EGFR (L861Q), EGFR (L858R/T790M), EGFR (d746-750), EGFR (d746-750/T790M), respectively. Oritinib can ...		EGFR
T1952	MK-2206 dihydrochloride	MK-2206 2HCl	Apoptosis , Akt , Autophagy
	MK-2206 dihydrochloride (MK-2206 2HCl) is a variant Akt inhibitor that inhibits Akt1, Akt2, and Akt3 (IC50=8/12/65 nM) with orally active, highly potent and selective potency. MK-2206 dihydrochloride exhibits antitumor a...		Apoptosis , Akt , Autophagy
T9997	GLL 398		Estrogen Receptor/ERR
	GLL 398 is an orally active and selective degrader of estrogen receptor with an IC50 of 1.14 nM. GLL 398 blocks tumor growth in xenograft breast cancer models.		Estrogen Receptor/ERR
T2705	Mutant EGFR inhibitor		EGFR
	Mutant EGFR inhibitor is a selective and potent Mutated EGFR inhibitor, inhibits L858R activating mutant, the Exonl9 deletion activating mutant and the T790M resistance mutant.		EGFR
T6918	Olmutinib	HM61713, BI 1482694,BI 1482694,HM61713	EGFR , BTK
	Olmutinib (HM61713, BI 1482694) is an orally available small molecule, a mutant-selective inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Olmutinib binds to and inhibits mutan...		EGFR , BTK
T3024	Avitinib	AC0010	EGFR , JAK , BTK
	Avitinib (AC0010), also known as AC0010 or AC0010MA, is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with potential antineoplastic activity. Upon oral administrat...		EGFR , JAK , BTK
T6949	PLX7904	PB04	Raf
	PLX7904 (PB04), also known as PB04, is a potent and selective paradox-breaker RAF inhibitor. It is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutan...		Raf
TQ0042	BAY-1436032		Dehydrogenase , Isocitrate Dehydrogenase (IDH)
	BAY-1436032 is a novel, selective and orally available inhibitor of pan-mutant isocitrate dehydrogenase 1 (IDH1).		Dehydrogenase , Isocitrate Dehydrogenase (IDH)
T21946	BIMU 8		5-HT Receptor
	BIMU 8 is a selective agonist of 5-HT4 with EC50s of 18 nM, 77 nM, and 540 nM for wild-type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4.		5-HT Receptor
T9224	CH5424802 analog		ALK
	CH5424802 analog is a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant.		ALK
T7326	6H05 (TFA)	6H05 TFA,6H05 trifluoroacetate	Ras
	6H05 TFA (6H05 trifluoroacetate) is a selective, and allosteric oncogenic mutant K-Ras(G12C) inhibitor.		Ras
T1809	AGI-6780		Dehydrogenase , Isocitrate Dehydrogenase (IDH)
	AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant.		Dehydrogenase , Isocitrate Dehydrogenase (IDH)
T6238	WZ4002		EGFR
	WZ4002 is a mutant-selective EGFR inhibitor for EGFR(L858R) and EGFR(T790M) with IC50 of 2 nM/8 nM.		EGFR
T71321	(S)-VU0637120		Others
	(S)-VU0637120 is a selective neuropeptide Y(4)R-mutant antagonist used in the study of metabolic disorders.		Others
T6008	CNX-2006	CNX 2006,CNX2006	EGFR
	CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.		EGFR
T62385	Befiradol hydrochloride	NLX-112 hydrochloride,F 13640 hydrochloride	5-HT Receptor
	Befiradol hydrochloride (NLX-112 hydrochloride) is a selective 5-hydroxytryptamine 1A (5-HT)1A receptor agonist with anxiolytic activity.Befiradol hydrochloride inhibits mutant ATXN3 aggregation.		5-HT Receptor