research use only
Cat.No.S8318
| Related Targets | PKC ROCK Bcr-Abl |
|---|---|
| Other TGF-beta/Smad Inhibitors | SB431542 RepSox (E-616452) Vactosertib (TEW-7197) LDN-193189 A-83-01 LDN-193189 Dihydrochloride Galunisertib (LY2157299) SRI-011381 (C381) LY2109761 SIS3 Hydrochloride |
| Molecular Weight | 232.32 | Formula | C15H20O2 |
Storage (From the date of receipt) | |
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| CAS No. | 546-43-0 | Download SDF | Storage of Stock Solutions |
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In vitro |
DMSO
: 46 mg/mL
(198.0 mM)
Ethanol : 46 mg/mL Water : Insoluble |
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In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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| Targets/IC50/Ki |
STAT3
activin/SMAD3
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| In vitro |
Alantolactone selectively suppresses STAT3 activation and exhibits potent anticancer activity in MDA-MB-231 cells. This compound effectively suppressed both constitutive and inducible STAT3 activation at tyrosine 705. It decreased STAT3 translocation to the nucleus, its DNA-binding, and STAT3 target gene expression. This chemical significantly inhibits STAT3 activation with a marginal effect on MAPKs and on NF-
kB transcription; however, this effect is not mediated by inhibiting STAT3 upstream kinases. SHP-1, SHP-2, and PTEN, which are protein tyrosine phosphatases (PTPs) were not affected by alantolactone. Its treatment resulted in the inhibition of migration, invasion, adhesion, and colony formation. It could induce activin signaling and activin target gene expression. This agent activated the activin signaling pathway in a cancer cell line. It could promote SMAD2/3 nuclear translocation in a very short time.
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| In vivo |
In vivo administration of alantolactone inhibited the growth of human breast xenograft tumors. This compound exerts no toxic effect on liver and kidneys in vivo. The drug was well tolerated by mice and no mortality or any sign of pharmacotoxicity was found at a dose of 100 mg/kg during all the experimental periods. It can cross blood-brain barrier.
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References |
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