AS 602801 (Bentamapimod)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
Size | Price | Stock |
---|---|---|
250mg | $650 | Check With Us |
500mg | $1050 | Check With Us |
1g | $1575 | Check With Us |
Cat #: V3732 CAS #: 848344-36-5 Purity ≥ 98%
Description: AS602801 (also known as Bentamapimod and PGL5001) is a novel, potent and ATP-competitive JNK (c-Jun N-terminal Kinase) inhibitor with IC50 values of 80 nM, 90 nM, and 230 nM for JNK1, JNK2, and JNK3, respectively.
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Molecular Weight (MW) | 457.55 |
---|---|
Molecular Formula | C25H23N5O2S |
CAS No. | 848344-36-5 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 10 mMr |
Water: N/Ar | |
Ethanol: N/A | |
SMILES Code | N#CC(C1=NC2=CC=CC=C2S1)C3=NC(OCC4=CC=C(CN5CCOCC5)C=C4)=NC=C3 |
Synonyms | AS602801; AS-602801; AS 602801; Bentamapimod; PGL5001; PGL-5001; PGL 5001 |
Protocol | In Vitro | Bentamapimod (AS 602801) treatment induces cell death and accordingly decreased the number of viable cells in all three cell lines in a dose-dependent manner, suggesting that Bentamapimod (AS 602801) may have selective cytotoxic activity against neoplastic cells. Bentamapimod (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. Bentamapimod (AS 602801) also inhibits the self-renewal and tumor-initiating capacity of cancer stem cells surviving Bentamapimod (AS 602801) treatment. |
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In Vivo | Treatment of nude mice bearing xenografts biopsied from women with endometriosis (BWE) with 30 mg/kg Bentamapimod (AS 602801) causes 29% regression of lesion. Medroxyprogesterone acetate (MPA) or progesterone (PR) alone did not cause regression of BWE lesions, but combining 10 mg/kg Bentamapimod (AS 602801) with MPA caused 38% lesion regression. In human endometrial organ cultures (from healthy women), treatment with Bentamapimod (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 + Bentamapimod (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 (AS 602801) reduces inflammatory cytokines in endometriotic lesions, while levels of cytokines in ipsilateral horns are unaffected. Furthermore, Bentamapimod (AS 602801) enhances natural killer cell activity, without apparent negative effects on uterus. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.1856 mL | 10.9278 mL | 21.8555 mL | 43.7111 mL |
5mM | 0.4371 mL | 2.1856 mL | 4.3711 mL | 8.7422 mL |
10mM | 0.2186 mL | 1.0928 mL | 2.1856 mL | 4.3711 mL |
20mM | 0.1093 mL | 0.5464 mL | 1.0928 mL | 2.1856 mL |
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Step Two: Enter the in vivo formulation
%DMSO
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%ddH2O
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Method for preparing DMSO master liquid:
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Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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