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Pulrodemstat (CC-90011) is an orally active, selective, and highly efficient lysine-specific demethylase-1 (LSD1) inhibitor with anticancer activity. It inhibits HNSCC cell proliferation and migration by triggering apoptosis and inhibiting head and neck squamous cell carcinoma growth.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $970 | 1-2 weeks |
Description | Pulrodemstat (CC-90011) is an orally active, selective, and highly efficient lysine-specific demethylase-1 (LSD1) inhibitor with anticancer activity. It inhibits HNSCC cell proliferation and migration by triggering apoptosis and inhibiting head and neck squamous cell carcinoma growth. |
Targets&IC50 | CD11b:7 nM (EC50), H209 cells (4 days):3 nM (EC50), H1417 cells (12 days):6 nM (EC50), Kasumi-1 cells:2 nM (EC50), H1417 cells (4 days):4 nM (EC50), LSD1:0.25 nM (IC50) |
In vitro | Pulrodemstat is a potent, selective, reversible and orally active lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 0.25 nM. [1] In the THP-1 cell line, Pulrodemstat strongly induced the expression of CD11b, a marker of target cell differentiation, with an EC50 value of 7 nM; furthermore, it showed antiproliferative effects in acute myeloid leukemia (AML) Kasumi-1 cells with an EC50 value of 2 nM. [1] After 4 days of treatment, Pulrodemstat reduced the levels of growth regulatory protein (GRP) in a dose-dependent manner. At pharmacologically effective concentrations, its EC50 was 3 nM and 4 nM for H209 and H1417 cells, respectively. significant antiproliferative effects were observed after 12 days of Pulrodemstat treatment of small cell lung cancer (SCLC) cells (EC50 of 6 nM for H1417), which were associated with GRP inhibition.[1] |
In vivo | In a patient-derived xenograft SCLC model, once-daily oral administration of 5 mg/kg of Pulrodemstat for 30 consecutive days significantly inhibited tumor growth. [1] Once-daily treatment with Pulrodemstat for 4 consecutive days resulted in a significant reduction in GRP mRNA levels in SCLC human tumor xenograft mice (H1417). Significant inhibition was observed at a dose of 2.5 mg/kg, with maximal effect at 5 mg/kg.[1] After intravenous administration of 5 mg/kg of Pulrodemstat, the systemic clearance was 32.4 mL/min/kg, the elimination half-life was 2 hours, and the volume of distribution was 7.5 L/kg. 5 mg/kg of Pulrodemstat was readily absorbed by the oral route, and it had an AUC0-24h of 1.8 μM-h, with a maximal concentration (Cmax) of 0.36 μM, and an oral bioavailability of 32%. [1] |
Alias | LSD1-IN-7, CC-90011, CC90011 |
Molecular Weight | 451.47 |
Formula | C24H23F2N5O2 |
Cas No. | 1821307-10-1 |
Smiles | N#CC1=CC=C(C=C1F)C=2N=C(N(C(=O)C2C=3C=CC(OC)=C(F)C3)C)N4CCC(N)CC4 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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