malignancies — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T12367	Parsaclisib	INCB050465	PI3K
	Parsaclisib (INCB050465) is a potent and selective inhibitor of PI3Kδ(IC50 of 1 nM at 1 mM ATP)		PI3K
T9715	Aplidine		SARS-CoV , DNA/RNA Synthesis
	Aplidine possesses antiviral activity against SARS-CoV-2(IC90 = 0.88 nM). Aplidine is a potent anti-cancer agent by targeting eukaryotic translation elongation factor 1 Alpha 2(EEF1A2, Kd = 80 nM).		SARS-CoV , DNA/RNA Synthesis
T12317	Orelabrutinib	ICP-022	BTK
	Orelabrutinib (ICP-022) is an orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK).		BTK
T6055	Quisinostat	JNJ-26481585	Apoptosis , HDAC , Autophagy
	Quisinostat (JNJ-26481585) (JNJ-26481585) is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against...		Apoptosis , HDAC , Autophagy
T12477	Uzansertib phosphate	INCB053914 phosphate	Pim
	Uzansertib phosphate (INCB053914 phosphate) is an orally active, ATP-competitive inhibitor of pan-PIM kinase(PIM1, PIM2, PIM3 with IC50s of 0.24 nM, 30 nM, 0.12 nM , respectively).		Pim
T6761	Ossirene	AS101	IL Receptor , Caspase , Interleukin
	Ossirene (AS101), a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.		IL Receptor , Caspase , Interleukin
T22349	JNJ-38158471	CS-2660	VEGFR , c-RET , c-Kit
	JNJ-38158471 (CS-2660), a highly selective, orally available, well tolerated VEGFR2 inhibitor with IC50 of 40 nM, inhibits closely related tyrosine kinases such as Ret and Kit with IC50 of 180 nM and 500 nM.		VEGFR , c-RET , c-Kit
T12311	Tirabrutinib hydrochloride	ONO-4059 (hydrochloride),GS-4059 (hydrochloride)	BTK
	Tirabrutinib hydrochloride (GS-4059 (hydrochloride)) is a selective and novelBTK with IC50 2.2 nm inhibitor.		BTK
T4976	Umbralisib	TGR-1202,RP5264,TGR 1202,TGR1202	PI3K
	Umbralisib (TGR 1202) is a PI3Kδ inhibitor.		PI3K
T0975	Chlorambucil	CB-1348,Chloroambucil,WR-139013	DNA Alkylator/Crosslinker , DNA Alkylation
	Chlorambucil (CB-1348) is an orally-active antineoplastic aromatic nitrogen mustard. Chlorambucil alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arr...		DNA Alkylator/Crosslinker , DNA Alkylation
T1038	Fludarabine	NSC 118218,Fludarabinum,F-ara-A	Apoptosis , Nucleoside Antimetabolite/Analog , DNA/RNA Synthesis , STAT
	Fludarabine (Fludarabinum) is a fluorinated purine analog, an inhibitor of nucleic acid synthesis and an inhibitor of STAT1 activation. Fludarabine has antitumor activity and can be used for the treatment of leukemia and...
T6079	NVP-ADW742	ADW742,ADW,GSK 552602A	Apoptosis , IGF-1R
	NVP-ADW742 (ADW) is an IGF-1R inhibitor with IC50 of 0.17 μM, >16-fold more potent against IGF-1R than InsR; little activity to HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit.		Apoptosis , IGF-1R
T12574	PTC299	Emvododstat,(4-chlorophenyl) (1S)-6-chloro-1-(4-methoxyphenyl)-1,3,4,9-tetrahydropyrido[3,4-b]indole-2-carboxylate	VEGFR , Dehydrogenase
	PTC299 ((4-chlorophenyl) (1S)-6-chloro-1-(4-methoxyphenyl)-1,3,4,9-tetrahydropyrido[3,4-b]indole-2-carboxylate) is an orally active inhibitor of VEGFA mRNA translation and selectively inhibits VEGF protein synthesis at t...		VEGFR , Dehydrogenase
T6104	Cerdulatinib hydrochloride	Cerdulatinib,PRT2070,PRT062070 hydrochloride,PRT062070,PRT2070 hydrochloride	MLK , c-Fms , Tyrosine Kinases , Hippo pathway , JAK , Syk
	Cerdulatinib hydrochloride (PRT2070 hydrochloride) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19...		MLK , c-Fms , Tyrosine Kinases , Hippo pathway , JAK , Syk
T6865	Quisinostat dihydrochloride	Quisinostat 2HCl,Quisinostat (JNJ-26481585) 2HCl,JNJ26854165(Quisinostat) 2HCl,JNJ-26481585 2HCl	Apoptosis , HDAC , Autophagy
	Quisinostat dihydrochloride (JNJ26854165(Quisinostat) 2HCl) is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, modest potent to HDACs 2, 4, 10, and 11; g...		Apoptosis , HDAC , Autophagy
T28297	Parsaclisib hydrochloride	Parsaclisib HCl,INCB-50465,INCB 050465,INCB-050465,INCB050465 HCl,INCB 50465,INCB50465 HCl	PI3K
	Parsaclisib hydrochloride (INCB050465 HCl) is a selectve PI3Kδ inhibitor with antitumor activity. Parsaclisib demonstrates potent activity with IC50 values ranging from 0.2 to 2 nM.		PI3K
T1601	Lomustine	CCNU,NSC 79037	Apoptosis , Others , DNA Alkylator/Crosslinker , DNA Alkylation , Autophagy
	Lomustine (NSC-79037) is an alkylating agent of value against both hematologic malignancies and solid tumors.
T10436	AZD4573		CDK
	AZD4573 is an effective and selective CDK9 inhibitor (IC50: <4 nM). It enables transient target engagement for the treatment of hematologic malignancies.		CDK
T23903	CM037	CM-037,A-37,CM 037,A37,A 37	Dehydrogenase
	CM037 (A-37) is a selective ALDH1A1 (acetaldehyde dehydrogenase 1A1) inhibitor (IC50; 4.6 µM) with antitumor activity and may be used in studies to eliminate gynecologic malignancies.		Dehydrogenase
TNU0014	1-(2-Deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil		Apoptosis
	1-(2-Deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil is a purine nucleoside analog with a broad spectrum of antitumor activity targeting inert lymphoid malignancies and inducing apoptosis.1-(2-Deoxy-2-fluoro-beta-D-arabino...		Apoptosis