hematologic

Plogosertib (CYC140) is an orally active, selective, potent, and ATP-competitive PLK1 inhibitor with an IC50 value of 3 nM.Plogosertib exhibits antiproliferative and anticancer activity and can be used for the study of solid and hematologic tumors. and hematologic tumors.

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

Efegatran is a hematologic agent and platelet aggregation inhibitor.

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

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.

Vincristine sulfate is an alkaloidal natural product that binds to microtubule proteins and inhibits the formation of microtubules, thereby inhibiting mitosis in tumor cells. Vincristine sulfate is used as a microtubule destabilizing agent in research studies for the treatment of hematologic neoplasms such as leukemias and lymphomas, as well as in studies related to sarcomas in children.

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.

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.

Uzansertib (INCB053914) is a potent ATP-competitive pan-PIM kinase inhibitor. It exhibits exceptional inhibitory activity against PIM1, PIM2, and PIM3 with IC50 values of 0.24 nM, 30 nM, and 0.12 nM, respectively. Furthermore, Uzansertib demonstrates significant anti-proliferative effects against an assorted range of hematologic tumor cell lines.

LP-284 is a potent DNA alkylating agent that kills solid tumors and can be used in hematologic cancer studies with compromised DNA repair, such as mantle cell lymphoma (MCL) [1] [2].

Idactamab (INT-001) is a monoclonal antibody to the human amino acid transport protein ASCT2.

Duvelisib, also known as IPI-145 and INK-1197, is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities. Upon administration, PI3K delta/gamma inhibitor IPI 145 prevents the activation of the PI3K delta/gamma-mediated signaling pathways which may lead to a reduction in cellular proliferation in PI3K delta/gamma-expressing tumor cells. Unlike other isoforms of PI3K, the delta and gamma isoforms are overexpressed primarily in hematologic malignancies and inflammatory and autoimmune diseases.

Fluindione is a hematologic drug.

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.

Plamotamab (XmAb-13676), a human bispecific antibody (bsAb) targeting CD3 and CD20, recruits cytotoxic T cells to eliminate CD20-expressing tumor cells. It demonstrates mild hematologic reaction (MR) and effectively induces tumor regression in vivo [1] [2].

KZR-616, a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 has the potential for the research of multiple autoimmune diseases[1][2]. KZR-616 also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). KZR-616 maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. KZR-616 (250 nM) shows a comparable cytokine inhibition profile peripheral blood mononuclear cells (PBMC)[1].KZR-616 is an immunoproteasome-selective inhibitor identified based on the optimization of ONX-0914 and PR-924 [3]. KZR-616 (5 mg/kg; i.v.; dosing was repeated on days 6, 8, 11, and 13) shows efficacy in the anticollagen antibody induced arthritis (CAIA) model[1]. [1]. Johnson HWB, et al. Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide). J Med Chem. 2018 Dec 27;61(24):11127-11143. [2]. Muchamuel T, et al. FRI0296 Kzr-616, a selective inhibitor of the immunoproteasome, blocks the disease progression in multiple models of systemic lupus erythematosus (SLE). Annals of the Rheumatic Diseases 2018;77:685. [3]. Xi J, et al. Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases. Eur J Med Chem. 2019;182:111646.

Molibresib besylate (GSK 525762C) is a selective and potent inhibitor of the bromodomain and extra-terminal (BET) family of proteins with potential anticancer activity for the study of refractory hematologic malignant diseases.Molibresib besylate generates reactive oxygen species (ROS), which potentiate ATM activation.

HT1042 is an inhibitor of the β5i component of the 20S proteasome complex, it is used to aid in the treatment of inflammatory diseases, autoimmune and hematologic malignancies.

Vincristine binds to tubulin and inhibits the formation of microtubules, thereby inhibiting mitosis of the cancer cell. Vincristine can be used as a microtubule-destabilizing agent for research on the treatment of hematologic cancers, such as leukemia and

KME-2780 is a potent, selective dual inhibitor of IRAK1 and IRAK4, suitable for research on dysregulation in innate immune signaling and hematologic malignancies [1].

CC-90002, a humanized anti-CD47 monoclonal antibody (mAb), demonstrates high affinity for CD47, characterized by a subnanomolar dissociation constant (K d). It is utilized in the research of hematologic malignancies and solid tumors [1] [2].

PI3Kδ γ-IN-1 is a selective and efficacious inhibitor of PI3Kδ γ, suitable for treating hematologic malignancies.

DB2115 (tertahydrochloride) is a powerful inhibitor of the myeloid master regulator PU.1. With significant potential in cancer research, particularly hematologic cancers like leukemia, as well as other conditions linked to PU.1 dysfunction, DB2115 (tertahydrochloride) offers promising avenues of study.

SBP-0636457 (SB1-0636457) is a SMAC mimetic and IAP inhibitor that specifically binds to the BIR-domains of IAP proteins with a Ki value of 0.27 μM, holding potential for research in solid tumors and hematologic cancers.

Golcadomide (CC-99282) is a orally active CRBN E3 ligase modulator that induces interactions between CRBN and its neo-substrate, recruiting the target disease-causing proteins and the E3 ubiquitin ligase.Golcadomide is used in the study of hematologic malignancies.

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 the post-transcriptional level. PTC299 is also a potent inhibitor of dihydrolactate dehydrogenase (DHODH).

Fosciclopirox disodium suppresses urothelial cancer growth by targeting the γ-secretase complex and selectively delivering the active metabolite, Ciclopirox, throughout the urinary tract. Ciclopirox demonstrates anticancer activity in various solid and hematologic malignancies [1] [2].

(Rac)-Lisaftoclax ((Rac)-APG-2575), a Bcl-2 inhibitor, is utilized in hematologic malignancy research (CN112898295A) [1].

Bcl-2-IN-11 (compound 6) is a potent and selective Bcl-2 activity inhibitor with an IC50 of 0.9 nM and minimal inhibition against Bcl-xl (IC50 > 1000 nM). It is used in cancer research related to Bcl-2 family protein overexpression, particularly in hematologic malignancies like acute lymphoid leukemia, while minimizing the risk of side effects such as thrombocytopenia [1] by sparing Bcl-xl.

Tubulin HDAC-IN-1 is a dual inhibitor of tubulin and HDAC8, interacting with tubulin via CH π interactions and with HDAC8 through hydrogen bonds. It effectively inhibits tubulin polymerization and selectively targets HDAC8 with an IC50 of 150 nM. Additionally, Tubulin HDAC-IN-1 demonstrates cytotoxicity against various human cancer cells, induces cell cycle arrest in the G2 M phase, and triggers cell apoptosis, making it valuable for studying hematologic and solid tumors, including neuroblastoma and leukemia [1].

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.

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).

Tefinostat (CHR-2845) is a potent monocyte macrophage-targeted histone deacetylase (HDAC) inhibitor that is cleaved to the active acid CHR-2847 by intracellular esterase human carboxylesterase-1 (hCE-1). Tefinostat exhibits antitumor activity and can be used in the study of leukemia and advanced hematologic malignancies.

KT-333 ammonium (Compound A) acts as a molecular glue that targets and promotes the degradation of the STAT3 protein through the ubiquitin-proteasome system. This compound achieves selective degradation by binding simultaneously to the STAT3 protein and the E3 ubiquitin ligase von Hippel-Lindau protein (VHL). It exhibits strong selectivity and efficacy in degrading STAT3, possessing notable antitumor properties. KT-333 ammonium is particularly useful for research on hematologic malignancies, including large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) [1].

Pidilizumab (CT-011), a humanized IgG1κ anti-PD-1 monoclonal antibody, serves as a DLL1 antagonist with potential applications in researching hematologic malignancies [1].

Anzurstobart (CC-95251; BMS-986351), a fully human monoclonal anti-SIRPα antibody with high affinity, inhibits the CD47-SIRPα interaction, potentiates macrophage-mediated phagocytosis of DLBCL cell lines in co-culture assays with Rituximab, and shows promise in solid and hematologic malignancy research [1].