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Cat. No. Product Name CAS No. Information
PC-36044

Glasdegib

1095173-27-5

Glasdegib (PF-04449913) is a potent, orally bioavailable smoothened (SMO) inhibitor with IC50 of 5 nM in the Gli-luciferase reporter assays, binds to human SMO (AA181-787) with IC50 of 4 nM; inhibits sonic hedgehog (Shh) stimulated luciferase expression in mouse embryonic fibroblasts with an IC50 of 6.8 nM, significantly reduces medulloblastoma growth in a Ptch1+/-p53+/- allograft model at doses that decreased murine Shh target gene expression; reduced downstream GLI2 protein and cell cycle regulatory gene expression in humanized stromal co-cultures and LSC (leukemia stem cells) xenografts.

Blood Cancer

Phase 3 Clinical

PC-35967

AP1903

195514-63-7

AP1903 (Rimiducid, AP-1903) is a potent, specific synthetic ligand of FKBP Phe36Val mutant (F36V-FKBP) with binding IC50 of 1.8 nM; displaces the Fluoresceinated FK506 probe from F36V-FKBP with an IC50 of 5 nM, but shows negligible binding activity to the wild-type protein; elicited potent and dose-dependent apoptotic death of human fibrosarcoma line HT1080 expressing dimerizer-dependent Fas constructs with EC50 of 0.1 nM; induces activation of Fas signaling both in vitro and in vivo, AP1903 is a lipid-permeant dimerizing ligand induced oligomerization and activation of FKBP.

Blood Cancer

Phase 3 Clinical

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

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