H1975 | TargetMol

カタログ番号	製品名	別名	ターゲット
T9552	BAZ1A-IN-1		Epigenetic Reader Domain
	BAZ1A-IN-1 is a potent BAZ1A inhibitor with the KD value of 0.52 μM for the BAZ1A bromodomain. BAZ1A-IN-1 shows good anti-survival activity against cancer cell lines with high BAZ1A expression, but weak or no activity ag...		Epigenetic Reader Domain
T9927	Panitumumab		EGFR
	Panitumumab is a fully human IgG2 monoclonal antibody targeting the epidermal growth factor receptor EGFR).		EGFR
T8151	Mobocertinib	tak788	EGFR
	Mobocertinib (tak788) is a potent inhibitor of epidermal growth factor receptor (EGFR) and an antineoplastic agent		EGFR
T16996	TAS6417		Apoptosis , EGFR
	TAS6417 is an EGFR inhibitor and is an efficacious drug candidate for patients with NSCLC (IC50: ranging from 1.1-8.0 nM).		Apoptosis , EGFR
T2490	Osimertinib	AZD-9291,Mereletinib	EGFR
	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 activi...		EGFR
T3634	Osimertinib mesylate	Mereletinib mesylate,AZD-9291 mesylate	EGFR
	Osimertinib mesylate (Mereletinib mesylate) is an irreversible and mutant selective EGFR inhibitor (IC50s: 12/1 nM for EGFR(L858R) and EGFR(L858R/T790M)).		EGFR
T21312	Afatinib	Afatinib free base,BIBW 2992	EGFR , Autophagy
	Afatinib (BIBW 2992) is an irreversible inhibitor of EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M and HER2 with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM , respectively).		EGFR , Autophagy
T6823	E3330		HIF/HIF Prolyl-Hydroxylase , DNA/RNA Synthesis
	E3330 is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.		HIF/HIF Prolyl-Hydroxylase , DNA/RNA Synthesis
T1773	Afatinib Dimaleate	BIBW2992,Afatinib,BIBW 2992MA2,Afatinib (BIBW2992) Dimaleate	EGFR , HER , Autophagy
	Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic act...		EGFR , HER , Autophagy
T22396	PF-6274484	PF 6274484	EGFR
	PF-6274484, a high affinity, irreversible covalent inhibitor of EGFR kinase with Ki of 0.14 nM, inhibits the autophosphorylation of wild-type EGFR in A549 cells and EGFRL858R/T790M in H1975 cells with IC50 of 5.8 nM and ...		EGFR
T60146	USP8-IN-1		DUB
	USP8-IN-1 is an inhibitor of USP8 with an IC 50 of 1.9 μM. USP8-IN-1 inhibits H1975 cell growth with a GI 50 of 82.04 μM [1].		DUB
T11157L	EGFR-IN-1 hydrochloride		EGFR
	EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R/T790M mutant EGFR with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride exhibits potent antitumor and antiproliferative activity...		EGFR
T63895	EGFR-IN-62
	EGFR-IN-62 is a potent inhibitor of EGFR kinase with IC50 values of 10 nM for L858R/T790 M, 29 nM for WT and 2 42 nM for L858R/T790 M/C797S. EGFR-IN-62 blocks the cell cycle of A549 and/or H1975 cells in G1/G0 phase and ...
T74351	PROTAC EGFR degrader 3		PROTACs
	PROTAC EGFR Degrader 3, a highly potent molecule, exhibits remarkable cellular activity against H1975 and HCC827 cells, maintaining high selectivity. It additionally reveals the lysosome's crucial role in the degradation...		PROTACs
T63531	HDAC6/HSP90-IN-1
	HDAC6/HSP90-IN-1 is a potent and selective dual inhibitor of HDAC6 (IC50: 4.3 nM) and HSP90 (IC50: 46.8 nM).HDAC6/HSP90-IN-1 downregulates PD-L1 expression in INF-γ-treated H1975 lung cancer cells.HDAC6/HSP90-IN-1 exhibi...
T63693	EGFR-IN-55
	EGFR-IN-55 is a potent inhibitor of EGFR, acting on EGFRWT (IC50: 70 nM) and EGFRL858R/T790M (IC50: 3.9 nM). EGFR-IN-55 was able to block the cell cycle of NCI-H1975 cells in G0/G1 phase, exhibiting anticancer effects.
T82491	EGFR-IN-90		EGFR
	EGFR-IN-90 (compound 34), an orally active EGFR inhibitor, demonstrates potent activity against EGFRL858R/T790M/C797S with an IC50 of 5.1 nM and effectively inhibits the proliferation of the H1975-TM cell line carrying E...		EGFR
T71436	D561-0775
	D561-0775 is a direct AMPK agonist, showing potential anti-cancer activity via inducing apoptosis, cell cycle arrest, suppressing glycolysis and cholesterol synthesis after activation of AMPK in gefitinib-resistant H1975...
T75100	DM-CO-(CH2)5-SMe
	DM-CO-(CH2)5-SMe, derived from an antibody-drug conjugate (ADC) metabolite, serves as an anticancer agent with demonstrated cytotoxicity against H1703, H1975, COLO704, and Colo720E cells [1].
T73128	EGFR-IN-61		EGFR
	EGFR-IN-61 (compound 22a), a potent EGFR kinase inhibitor, exhibits IC50 values of 42 nM for L858R/T790M, 137 nM for L858R/T790M/C797S, and 743 nM for WT. Additionally, it demonstrates antiproliferative activity against ...		EGFR
T79393	ALK/EGFR-IN-2
	ALK/EGFR-IN-2 is a potent dual inhibitor targeting ALK and EGFR, promoting apoptosis and G0/G1 cell cycle arrest in cancer cells. It effectively suppresses proliferation in H1975, PC9, and Baf3-EML4-ALK cancer cell lines...
T79394	ALK/EGFR-IN-3
	ALK/EGFR-IN-3 is a dual ALK and EGFR inhibitor that demonstrates potent anti-proliferative effects on various cancer cell lines, including H1975, PC9, and Baf3-EML4-ALK, with respective IC50 values of 0.1360, 0.0332, and...
T75261	EGFR-IN-1 TFA
	EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR . EGFR-I...
T74515	PROTAC EGFR degrader 4
	PROTAC EGFR degrader 4 is a potent molecule designed to target and degrade mutant EGFR, showcasing its effectiveness by inducing degradation of EGFR del19 and EGFR L858R/T790M with DC50 values of 0.51 nM and 126 nM, resp...
T11157	EGFR-IN-1		EGFR
	EGFR-IN-1, an orally active and irreversible selective inhibitor targeting L858R/T790M mutant EGFR, exhibits strong antiproliferative and antitumor activity, particularly against H1975 cells and first line mutant HCC827 ...		EGFR
T79388	Anticancer agent 154		Reactive Oxygen Species
	Anticancer agent 154 (Compound 8h) enhances reactive oxygen species production, causing mitochondrial damage, and promotes cell apoptosis and DNA damage. It triggers ferroptosis by depleting GSH, diminishing GPX4 express...		Reactive Oxygen Species
T74880	Cys-McMMAF
	Cys-McMMAF, the active compound liberated from AlMcMMAF—a humanized anti-5T4 A1 antibody connected to the microtubule-disrupting molecule MMAF through a maleimidocaproyl linker—demonstrates antitumor effectiveness in two...
T74623	PROTAC EGFR degrader 7
	PROTAC EGFR degrader 7 (compound 13b) is a potent, selective CRBN-recruiting agent targeting EGFR L858R/T790M mutations with a DC50 of 13.2 nM. It effectively inhibits proliferation in NCI–H1975 cells with an IC50 of 46....
T79152	PROTAC EGFR degrader 8		EGFR
	PROTAC EGFR degrader 8 (T-184) is a PROTAC that selectively degrades the epidermal growth factor receptor (EGFR) with a DC50 of 15.56 nM in HCC827 cells. It effectively inhibits the growth of various cell lines, includin...		EGFR
T79214	Tubulin/AKT1-IN-1		Akt
	Tubulin/AKT1-IN-1 (Compound D1-1) serves as an inhibitor of both tubulin polymerization and AKT pathway activation, effectively suppressing proliferation and metastasis of H1975 cells while modestly inducing apoptosis. T...		Akt
T63769	EGFR-IN-60
	EGFR-IN-60 is an effective, orally active, safe antitumor agent. EGFR-IN-60 significantly inhibits EGFRWT (IC50: 83 nM), EGFRT790M (IC50: 26 nM), EGFRL858R (IC50: 53 nM) and JAK3 (IC50: 69 nM). IN-60 inhibited H1975 cell...
T81380	PROTAC EGFR degrader 7 diTFA		PROTACs
	PROTAC EGFR degrader 7 (compound 13b) is a potent, selective, CRBN-recruiting EGFRL858R/T790M degrader with a DC50 of 13.2 nM. It effectively inhibits proliferation of NCI-H1975 cells with an IC50 of 46.82 nM, induces ap...		PROTACs
T79392	ALK/EGFR-IN-1		EGFR
	ALK/EGFR-IN-1 (Compound 8l) is a dual inhibitor targeting both ALK and EGFR, effectively blocking their phosphorylation. It demonstrates potent inhibition of ALK/EGFR mutants with IC50 values of 4.3 nM for EGFR L858R T79...		EGFR
T72784	OTUB1/USP8-IN-1		DUB
	OTUB1/USP8-IN-1 is a potent OTUB1/USP8 inhibitor with potential anticancer activity, with IC50 values of 0.17 and 0.28 nM for OTUB1 and USP8, respectively.OTUB1/USP8-IN-1 can be used in the study of non-small-cell lung c...		DUB
T79368	Antiproliferative agent-34		EGFR
	Antiproliferative Agent-34 (Compound A14), a multitarget kinase inhibitor, demonstrates IC50 values of 177 nM for EGFR L858R/T790M and 1567 nM for EGFR WT. Additionally, it inhibits JAK2, ROS1, FLT3, FLT4, and PDGFRα wit...		EGFR
T83890	Flavokawain 1i	Flavokavain 1i
	Flavokawain 1i, a derivative of chalcones flavokawain A, flavokawain B, and flavokawain C, exhibits anticancer and antiviral properties. At a concentration of 30 µM, it suppresses the growth of gefitinib-resistant H1975 ...
T35897	ASK120067
	ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1]...
T16492	PF-06459988		EGFR
	PF-06459988 is a novel, effective, orally active, irreversible, and selective epidermal growth factor receptor (EGFR) mutant inhibitor. PF-06459988 has high efficiency and high affinity for EGFRs double mutants containin...		EGFR
T6734	WZ8040		EGFR
	WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).		EGFR

Compounds

BAZ1A-IN-1

T9552

Synonym:

Target: Epigenetic Reader Domain

Target: Apoptosis, EGFR

Osimertinib

T2490

Synonym: AZD-9291,Mereletinib

Target: EGFR

Osimertinib mesylate

T3634

Synonym: Mereletinib mesylate,AZD-9291 mesylate

Target: EGFR

Afatinib

T21312

Synonym: Afatinib free base,BIBW 2992

Target: EGFR, Autophagy

E3330

T6823

Synonym:

Target: HIF/HIF Prolyl-Hydroxylase, DNA/RNA Synthesis

Afatinib Dimaleate

T1773

Synonym: BIBW2992,Afatinib,BIBW 2992MA2,Afatinib (BIBW2992) Dimaleate

Target: EGFR, HER, Autophagy

EGFR-IN-1 hydrochloride

PROTAC EGFR degrader 3

PROTAC EGFR degrader 4

Target: Reactive Oxygen Species

PROTAC EGFR degrader 7

T74623

Synonym:

Target:

PROTAC EGFR degrader 8

PROTAC EGFR degrader 7 diTFA

Antiproliferative agent-34

Synonym: Flavokavain 1i

カタログ番号	製品名	別名	ターゲット
TN2755	2-Desoxy-4-epi-pulchellin		Anti-infection
	2-Desoxy-4-epi-pulchellin has potent in vitro cytotoxicities against the K562, MCF-7, Hela, DU145, U937, H1975, SGC-7901, A549, MOLT-4, and HL60 cell lines with IC50 values ranging from 0.10 to 46.7uM, while it shows sig...		Anti-infection

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阻害剤

天然化合物

Compounds

天然物製品