A multi-kinase inhibitor
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RGB-286638

Item No. 29499

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
CAS Number
784210-88-4
Molecular Formula
C29H35N7O4
Formula Weight
545.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:20): 0.05 mg/mlEthanol: Partially soluble
λmax
234, 274, 367 nm
SMILES
O=C1C2=C(NN=C2C3=CC=C(CN4CCN(CCOC)CC4)C=C3)C5=C1C(NC(NN6CCOCC6)=O)=CC=C5
InChi Code
InChI=1S/C29H35N7O4/c1-39-16-13-34-9-11-35(12-10-34)19-20-5-7-21(8-6-20)26-25-27(32-31-26)22-3-2-4-23(24(22)28(25)37)30-29(38)33-36-14-17-40-18-15-36/h2-8H,9-19H2,1H3,(H,31,32)(H2,30,33,38)
InChi Key
XLSYZSRXVVCHLS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    100 mg

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    Product Description

    RGB-286638 is a multi-kinase inhibitor.1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cirstea, D., Hideshima, T., Santo, L., et al. Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. Leukemia 27(12), 2366-2375 (2013).