A multi-kinase inhibitor
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ACTB-1003

Item No. 30069

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
CAS Number
939805-30-8
Molecular Formula
C27H26F5N7O3
Formula Weight
591.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.33 mg/mlEthanol: 1 mg/ml
SMILES
NC1=NC=NN2C1=C(C3=CC(F)=C(NC(NC4=CC(C(F)(F)F)=CC=C4F)=O)C=C3)C(COC)=C2CN5CCOCC5
InChi Code
InChI=1S/C27H26F5N7O3/c1-41-13-17-22(12-38-6-8-42-9-7-38)39-24(25(33)34-14-35-39)23(17)15-2-5-20(19(29)10-15)36-26(40)37-21-11-16(27(30,31)32)3-4-18(21)28/h2-5,10-11,14H,6-9,12-13H2,1H3,(H2,33,34,35)(H2,36,37,40)
InChi Key
GZPJCJKUZPUFAL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    ACTB-1003 is a multi-kinase inhibitor (IC50s = 6, 2, 4, 5, and 32 nM for FGFR1, VEGFR2, Tie-2, RSK, and p70S6K, respectively).1 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).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Patel, K., Fattaey, A., and Burd, A. ACTB-1003: An oral kinase inhibitor targeting cancer mutations (FGFR), angiogenesis (VEGFR2, TEK), and induction of apoptosis (RSK and p70S6K). J. Clin. Oncol. 28(15_suppl), e13665-e13665 (2010).