A multi-kinase inhibitor (IC50s = 6

ACTB-1003 – 10 mg

Brand:
Cayman
CAS:
939805-30-8
Storage:
-20
UN-No:
Non-Hazardous - /

ACTB-1003 is a multi-kinase inhibitor (IC50s = 6, 2, 4, 5, and 32 nM for FGFR1, VEGFR2, Tie-2, RSK, and p70S6K, respectively).{49609} It inhibits growth of OPM2 human multiple myeloma and murine Ba/F3-TEL-FGFR1 leukemia cells in vitro. ACTB-1003 inhibits tumor angiogenesis in an H460 mouse xenograft model. It also reduces tumor growth in an HCT116 mouse xenograft model when administered in combination with 5-fluorouracil (5-FU; Item No. 14416) or paclitaxel (Item No. 10461).  

 

Available on backorder

Add to quotes
SKU: 30069 - 10 mg Category:

Description

A multi-kinase inhibitor (IC50s = 6, 2, 4, 5, and 32 nM for FGFR1, VEGFR2, Tie-2, RSK, and p70S6K, respectively); inhibits growth of OPM2 human multiple myeloma and murine Ba/F3-TEL-FGFR1 leukemia cells in vitro; inhibits tumor angiogenesis in an H460 mouse xenograft model; reduces tumor growth in an HCT116 mouse xenograft model when administered in combination with 5-FU or paclitaxel

Formal name: N-[4-[4-amino-6-(methoxymethyl)-7-(4-morpholinylmethyl)pyrrolo[2,1-f][1,2,4]triazin-5-yl]-2-fluorophenyl]-N′-[2-fluoro-5-(trifluoromethyl)phenyl]-urea

Synonyms: 

Molecular weight: 591.5

CAS: 939805-30-8

Purity: ≥98%

Formulation: A crystalline solid

Related products

  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 50 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 50 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 1 mg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 1 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 25 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 25 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 100 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 100 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page