Bentamapimod, also known as AS602801, is an ATP-competitive JNK inhibitor with IC50 of 80 nM, 90 nM, and 230 nM for JNK1, JNK2, and JNK3, respectively. AS 602801 exhibits cytotoxicity against both serum-cultured non-stem cancer cells and cancer stem cells derived from human pancreatic cancer, non-small cell lung cancer, ovarian cancer and glioblastoma at concentrations that did not decrease the viability of normal human fibroblasts. AS 602801 also inhibits the self-renewal and tumor-initiating capacity of cancer stem cells surviving AS 602801 treatment.
In vivo: Bentamapimod (30 mg/kg) on nude mice bearing xenografts biopsied from women with endometriosis (BWE) causes 29% regression of lesion. In human endometrial organ cultures (from healthy women), treatment with AS-602801 or MPA reduced matrix metalloproteinase-3 (MMP-3) release into culture medium. In organ cultures established with BWE, PR or MPA failed to inhibit MMP-3 secretion, whereas AS 602801 alone or MPA + AS 602801 suppresses MMP-3 production. In an autologous rat endometriosis model, AS 602801 causes 48% regression of lesions compared to GnRH antagonist Antide (84%). Bentamapimod reduces inflammatory cytokines in endometriotic lesions, while levels of cytokines in ipsilateral horns are unaffected.
| Cell Experiment | |
|---|---|
| Cell lines | PANC-1, A2780, and A549 human cancer cells |
| Preparation method | Bentamapimod (AS602801) is dissolved in DMSO (10 mM) and stored, and then diluted with appropriate media before use. PANC-1, A2780, and A549 human cancer cells and IMR90 human normal fibroblasts are treated without (control) or with the indicated concentrations of AS 602801 (2.5, 5, and 7.5 μM) for 3 days. The number of viable cells (left panels) and the percentage of dead cells (right panels) are determined using trypan blue as a vital dye. |
| Concentrations | 2.5, 5, and 7.5 μM |
| Incubation time | 3 days |
| Animal Experiment | |
|---|---|
| Animal models | 5-week-old athymic (ncr/nude) ovariectomized mice |
| Formulation | dissolved in in DMSO (10 mM) and diluted with PBS |
| Dosages | 10 mg/kg and 30 mg/kg/animal for 30 days |
| Administration | gavage |
| Molecular Weight | 457.55 |
| Formula | C25H23N5O2S |
| CAS Number | 848344-36-5 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related JNK Products |
|---|
| JIP-1(153-163)
JIP-1(153-163) (TI-JIP) is a peptide inhibitor of c-JNK, based on residues 153-163 of JNK-interacting protein-1 (JIP-1) (Modifications: Phe-11 = C-terminal amide). |
| JNK3 inhibitor-5
JNK3 inhibitor-5 is a potent and selective JNK3 inhibitor with an IC50 of 0.379 nM. |
| JNK-1-IN-1
JNK-1-IN-1 is a JNK-1 inhibitor. |
| JNK2-IN-1
JNK2-IN-1 is a JNK2 inhibitor (Kds: 79.2 μM). |
| JNK-1-IN-2
JNK-1-IN-2 is a JNK-1 inhibitor (IC50: 33.5 nM). |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
