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Bentamapimod

Cat. No. M8921
Bentamapimod Structure
Synonym:

AS-602801

Size Price Availability Quantity
5mg USD 200 In stock
10mg USD 300 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 457.55
Formula C25H23N5O2S
CAS Number 848344-36-5
Purity >98%
Solubility DMSO 10 mM
Storage at -20°C
References

The novel JNK inhibitor AS602801 inhibits cancer stem cells in vitro and in vivo.
Okada M, et al. Oncotarget. 2016 May 10;7(19):27021-32. PMID: 27027242.

c-Jun NH2-terminal kinase inhibitor bentamapimod reduces induced endometriosis in baboons: an assessor-blind placebo-controlled randomized study.
Hussein M, et al. Fertil Steril. 2016 Mar;105(3):815-824.e5. PMID: 26654972.

Bentamapimod (JNK Inhibitor AS602801) Induces Regression of Endometriotic Lesions in Animal Models.
Palmer SS, et al. Reprod Sci. 2016 Jan;23(1):11-23. PMID: 26335175.

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  Catalog
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Keywords: Bentamapimod, AS-602801 supplier, JNK, inhibitors

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