malignancies

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.

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 HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7.

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; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. Phase 2.

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 lymphoma.

A-485 is a potent and selective catalytic p300 CBP inhibitor with IC50 values of 9.8 nM for p300 and 2.6 nM for CBP.

R306465 (JNJ-16241199) is an orally active and selective class I histone deacetylase (HDAC 1) inhibitor with an IC50 of 3.3 nM. R306465 has a broad spectrum of antitumor activity, can induce histone 3 acetylation, and induce apoptosis, and can be used to study solid tumors and hematological malignancies.

QL-X-138 is a potent and selective BTK and MNK dual kinase inhibitor that binds covalently to BTK and non-covalently to MNK. The IC50 values of QL-X-138 are 9.4 nM for BTK, 107.4 nM for MNK1, 26 nM for MNK2, and 3.5 μM against Dengue 2. QL-X-138 is used in the study of B-cell malignancies and B-cell malignant tumors.

MU1656 is a potent and selective inhibitor of histone methyltransferase DOT1L (IC50 = 2 nM), a key epigenetic regulatory protein involved in the development of cancers such as hematologic malignancies, thus MU1656 was able to significantly inhibit the proliferation of cancer cells and induce apoptosis.

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 arrest, and apoptosis.

Lomustine (NSC-79037) is an alkylating agent of value against both hematologic malignancies and solid tumors.

Acalabrutinib (ACP-196), also known as ACP-196, is an orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, ACP-196 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.

Sonrotoclax TFA is an orally available and highly potent and selective Bcl-2 inhibitor of WT and G101V mutants with antitumor activity for the study of hematologic malignancies.

GDC-0425 (RG-7602) is an orally administered, selective small molecule inhibitor of checkpoint kinase 1 (ChK1), used in research on various malignancies [1] [2].

AZD1480 is a novel ATP-competitive JAK2 inhibitor (IC50: 0.26 nM), selectivity act against Tyk2 and JAK3, and to a smaller extent against JAK1. AZD1480 has been used in trials studying the treatment of Solid Malignancies, Post-Polycythaemia Vera, Primary

Ossirene (AS101), a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.

Satraplatin (BMS182751) is an orally available antineoplastic platinum(IV) complex.Satraplatin has a favorable toxicity profile and appears to have clinical activity against a variety of malignancies.

GAC0003A4 is a potent LXR inverse agonist with antitumor activity that inhibits the transcription of LXR proteins.GAC0003A4 degrades LXRβ proteins and inhibits the proliferation of PDAC cells in a dose-dependent manner.GAC0003A4 has been used in the study of advanced pancreatic cancers and other recalcitrant malignancies.

AZD4573 is an effective and selective CDK9 inhibitor (IC50: <4 nM). It enables transient target engagement for the treatment of hematologic malignancies.

HDACs mTOR Inhibitor 1 is a dual HDAC and mammalian target of Rapamycin (mTOR) inhibitor for treating hematologic malignancies, with IC50 values of 0.19 nM, 1.8 nM, 1.2 nM, and >500 nM for HDAC1, HDAC6, mTOR, and PI3Kα, respectively.

Ibrutinib-MPEA is ibrutinib derivative. Ibrutinib is a covalent and irreversible BTK inhibitor that has been used to treat hematological malignancies.

Tirabrutinib hydrochloride is a potent, highly selective, and irreversible oral BTK inhibitor. Tirabrutinib hydrochloride irreversibly covalently binds to Bruton tyrosine kinase (BTK) in B cells and exhibits potent in vitro cytotoxicity against many types of B cell malignancies, as well as in vivo antitumor activity in mouse models [1].

Orelabrutinib (ICP-022) is an orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK).

Parsaclisib (INCB050465) is a potent and selective inhibitor of PI3Kδ(IC50 of 1 nM at 1 mM ATP)

Penitrem A is a selective antagonist of BK channel with antiproliferative and anti-invasive activities against multiple malignancies.