A dual inhibitor of Aurora kinases and FLT3
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CCT241736

Item No. 26185

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-chloro-7-[4-[(4-chlorophenyl)methyl]-1-piperazinyl]-2-(1,3-dimethyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine
CAS Number
1402709-93-6
Molecular Formula
C22H23Cl2N7
Formula Weight
456.4
Purity
≥90%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10mg/mLDMF:PBS (pH 7.2) (1:2): 0.3mg/mLDMSO: 2mg/mL
λmax
218, 256, 310 nm
SMILES
ClC1=CN=C(N=C(C2=CN(C)N=C2C)N3)C3=C1N4CCN(CC5=CC=C(Cl)C=C5)CC4
InChi Code
InChI=1S/C22H23Cl2N7/c1-14-17(13-29(2)28-14)21-26-19-20(18(24)11-25-22(19)27-21)31-9-7-30(8-10-31)12-15-3-5-16(23)6-4-15/h3-6,11,13H,7-10,12H2,1-2H3,(H,25,26,27)
InChi Key
AKJBLKUZXRMECW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

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    Product Description

    CCT241736 is a dual inhibitor of Aurora kinases (Kds = 7.5 and 48 nM for Aurora A and B, respectively) and FLT3 (Kds = 6.2, 38, and 14 nM for wild-type, FLT3ITD, and FLT3D835Y, respectively).1 It also inhibits the activity of 22 additional kinases by greater than 90% in a panel of 386 nonmutant kinases at 1 µM. CCT241736 inhibits cell growth of SW620, HCT116, MOLM-13, and MV4-11 cancer cells (GI50s = 1, 0.3, 0.1, and 0.3 µM, respectively). Oral administration of CCT241736 (50 mg/kg twice per day) reduces tumor growth by 58% in an MV4-11 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bavetsias, V., Crumpler, S., Sun, C., et al. Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: Identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia. J. Med. Chem. 55(20), 8721-8734 (2012).