Home>>Signaling Pathways>> Cancer Biology>>1,2,3,4-Tetrahydrostaurosporine

1,2,3,4-Tetrahydrostaurosporine (Synonyms: AFN-941)

Catalog No.GC46039

A mutant EGFR inhibitor

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1,2,3,4-Tetrahydrostaurosporine Chemical Structure

Cas No.: 220038-19-7

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1mg
$796.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

1,2,3,4-Tetrahydrostaurosporine is a derivative of staurosporine and an inhibitor of mutant EGFR (IC50 = 74 nM for EGFRT790M).1 It is selective for EGFRT790M over wild-type EGFR (IC50 = 390 nM). It also binds to Janus kinase 3 (JAK3).2

|1. Song, X., Liu, X., and Ding, X. Staurosporine scaffold-based rational discovery of the wild-type sparing reversible inhibitors of EGFR T790M gatekeeper mutant in lung cancer with analog-sensitive kinase technology. J. Mol. Recognit. 30(4), (2017).|2. Boggon, T.J., Li, Y., Manley, P.W., et al. Crystal structure of the Jak3 kinase domain in complex with a staurosporine analog. Blood 106(3), 996-1002 (2005).

Chemical Properties

Cas No. 220038-19-7 SDF
Synonyms AFN-941
Canonical SMILES [H][C@]12N(C3=C4C5=C(CNC5=O)C6=C3N([C@](O2)(C)[C@H](OC)[C@H](NC)C1)C7=CC=CC=C76)C8=C4CCCC8
Formula C28H30N4O3 M.Wt 470.6
Solubility Acetone: slightly soluble,DMSO: slightly soluble Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.1249 mL 10.6247 mL 21.2495 mL
5 mM 0.425 mL 2.1249 mL 4.2499 mL
10 mM 0.2125 mL 1.0625 mL 2.1249 mL
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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. )

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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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Average Rating: 5 ★★★★★ (Based on Reviews and 38 reference(s) in Google Scholar.)

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