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Cat. No. Product Name CAS No. Information
PC-35328

ARQ-531

2095393-15-8

ARQ-531 (ARQ531) is a potent, reversible, orally available inhibitor of both wild type and C481S-mutant BTK kinase with IC50 of 0.85 and 0.39 nM, respectively; also ptently inhibits 45 kinases with >50% inhibition at 200 nM (TEC, BMX, LCK, TRK family kinases etc.); does not require the C481S residue to bind to BTK, inhibits CD69 expression on CD20+ B-cells with IC50 of 42 nM (Ibrutinib, IC50=3 nM); ARQ-531 inhibits proliferation of malignant cells both sensitive and resistant to ibrutinib (SUDHL6 Cell GI50=80 nM), ARQ 531 is superior to Ibrutinib in a TCL1 highly predictive adoptive transfer model of CLL.

Blood Cancer

Phase 1 Clinical

PC-35205

IACS-010759

1570496-34-2

IACS-010759 (IACS010759) is a small molecule inhibitor of mitochondrial oxidative phosphorylation (OXPHOS), targets complex I of the mitochondrial electron transport chain; decreases cell viability and increases apoptosis with EC50 values between 1 nM-50 nM across multiple lines; robustly inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS, reduces aspartate production that leads to impaired nucleotide biosynthesis; potently inhibits tumor growth of brain cancer and AML in vivo.

Blood Cancer

Phase 1 Clinical

PC-63502

S55746

1448584-12-0

S55746 (BCL201, Servier-1) is a novel potent, selective, orally bioavailable inhibitor of BCL-2 with Ki of 1.3 nM, 70- 400 fold selectivity over BCL-XL, on significant binding to MCL-1 and BFL-1; potently induces RS4;11 cell killing after 72 h of treatment with an IC50 of 71.6 nM, exhibits a much weaker activity in H146 (IC50 1.7 μM), a BCL-XL-dependent cell line; concentration-dependently disrupts the BCL-2/BAX complex in RS4;11 cells, selectively induces apoptosis through BCL-2 inhibition in a BAX/BAK-dependent manner; induces cell death in a panel of non-Hodgkin lymphoma cells; inhibits xenograft growth in RS4;11 and Toledo models.

Blood Cancer

Phase 1 Clinical

PC-63391

ASTX660

1799328-86-1

ASTX660 is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM; potently inhibits association between XIAP and caspase 9 in HEK293 cell line with EC50 of 2.8 nM, binds to and leads to the degradation of cIAP1/2 and stabilisation of NIK in cell; induces apoptosis in MDA-MB-231 cells with EC50 of 1.8 nM, which is TNF-α-dependent; inhibits tumor growth in mice bearing breast and melanoma tumor xenografts.

Blood Cancer

Phase 2 Clinical

PC-63366

ETC-206

1464151-33-4

ETC-206 (ETC-1907206) is a novel potent, selective MNK1/2 inhibitor with IC50 of 64/86 nM, inhibits eIF4E phosphorylation inhibition in HeLa cell line with IC50 of 321 nM; displays excellent kinase selectivity, inhibits only 2 kinases by >65% at 1 uM against a panel of 104 kinases; demonstrates potent anti-proliferative activity against 25 hematological cancer cell lines with submicromolar IC50, especially against GK-5, DOHH2, AHH1 and P3HR-1 cell lines; prevents BC CML LSC self-renewal in vitro, significantly enhances the anti-tumor activity of dasatinib in BC CML mouse xenograft model.

Blood Cancer

Phase 1 Clinical

PC-43332

CC-401 hydrochloride

1438391-30-0

CC-401 hydrochloride is a potent, selective, ATP-competitive pan-JNK inhibitor with Ki of 25-50 nM, displays >40-fold selectivity over other related kinases, including p38, ERK, IKK2, PK C, Lck, and ZAP70; decreases hepatic necrosis and apoptosis after orthotopic liver transplantation in vivo; blocks JNK signaling in the rat obstructed kidney and significantly inhibits renal fibrosis in terms of interstitial myofibroblast accumulation and collagen IV deposition, also significantly reduces tubular apoptosis in the obstructed kidney; sensitizes hypoxic colon cancer cells to DNA-damaging agents, potentiates the effect of bevacizumab and oxaliplatin in HT29-derived mouse xenografts.

Blood Cancer

Phase 1 Discontinued

PC-43206

ORY-1001 trans and cis isomers

1431326-61-2

ORY-1001 (RG-6016) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM, displays high selectivity for KDM1A over other FAD-containing monoamine oxidases; exhibits low nanomolar cellular activity (EC50 < 1 nM) in the THP1 differentiation assay and induces the CD11b marker within 6 hr of treatment in FACS based differentiation assay in THP1 cell line; induces H3K4me2 accumulation on KDM1A target genes, blast differentiation, and reduction of leukemic stem cell capacity in AML; exhibits potent synergy with standard-of-care drugs and selective epigenetic inhibitors, reduces growth of AML xenograft models.

Blood Cancer

Phase 2 Clinical

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