A multi-kinase inhibitor; inhibits a variety of kinases

RGB-286638 – 100 mg

Brand:
Cayman
CAS:
784210-88-4
Storage:
-20
UN-No:
Non-Hazardous - /

RGB-286638 is a multi-kinase inhibitor.{47793} It inhibits a variety of kinases, including cyclin-dependent kinase 1 (CDK1), CDK2-7 and CDK9, as well as the tyrosine kinases FMS, JAK2, and c-Src and the serine/threonine kinases GSK3β, TAK1, JNK1A1, JNK1A2, AMPK, and MEK1 (IC50s = 1-55 nM). RGB-286638 inhibits proliferation of multiple myeloma cancer cell lines endogenously expressing mutant and wild-type p53 (EC50s = 20-70 nM), as well as patient-derived multiple myeloma cells when used at concentrations of 50 and 100 nM. It induces G1/S and G2/M cell cycle arrest and apoptosis of MM.1S human multiple myeloma cells when used at a concentration of 50 nM. RGB-286638 decreases tumor growth in an MM.1S mouse xenograft model when administered at doses of 30 and 40 mg/kg per day for 14 days.  

 

Available on backorder

Add to quotes
SKU: 29499 - 100 mg Category:

Description

A multi-kinase inhibitor; inhibits a variety of kinases, including CDK2-7 and CDK9, FMS, JAK2, c-Src, GSK3β, TAK1, JNK1A1, JNK1A2, AMPK, and MEK1 (IC50s = 1-55 nM); inhibits proliferation of multiple myeloma cancer cell lines endogenously expressing mutant and wild-type p53 (EC50s = 20-70 nM), as well as patient-derived multiple myeloma cells at 50 and 100 nM; induces G1/S and G2/M cell cycle arrest and apoptosis of MM.1S human multiple myeloma cells at 50 nM; decreases tumor growth in an MM.1S mouse xenograft model at 30 and 40 mg/kg per day for 14 days

Formal name: N-[1,4-dihydro-3-[4-[[4-(2-methoxyethyl)-1-piperazinyl]methyl]phenyl]-4-oxoindeno[1,2-c]pyrazol-5-yl]-N′-4-morpholinyl-urea

Synonyms: 

Molecular weight: 545.6

CAS: 784210-88-4

Purity: ≥98%

Formulation: A crystalline solid

Related products

  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 100 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 - 100 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 – 5 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 - 5 mg

    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
  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 25 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 25 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page