A potent inhibitor of Cdc7
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XL413 (hydrochloride)

Item No. 24906

Technical Information
Formal Name
8-chloro-2-(2S)-2-pyrrolidinyl-benzofuro[3,2-d]pyrimidin-4(3H)-one, monohydrochloride
CAS Number
2062200-97-7
Molecular Formula
C14H12ClN3O2 • HCl
Formula Weight
Purity
≥98%
A crystalline solid
DMSO: 0.2 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
232, 289 nm
SMILES
O=C1N=C([C@@H]2CCCN2)NC3=C1OC4=C3C=C(Cl)C=C4.Cl
InChi Code
InChI=1S/C14H12ClN3O2.ClH/c15-7-3-4-10-8(6-7)11-12(20-10)14(19)18-13(17-11)9-2-1-5-16-9;/h3-4,6,9,16H,1-2,5H2,(H,17,18,19);1H/t9-;/m0./s1
InChi Key
UNDKJUKLBNARIZ-FVGYRXGTSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    XL413 is a potent inhibitor of Cdc7 (IC50 = 3.4 nM).1 It is >60, >10, and >300-fold selective for Cdc7 over CK2, PIM1, and a panel of over 100 protein kinases, respectively. XL413 inhibits the growth of MDA-MB-231T and COLO 205 cells (IC50s = 118 and 140 nM, respectively). It inhibits Cdc7-specific phosphorylation of mini-chromosome maintenance protein (MCM2) and induces cell cycle accumulation in the S and G2 phases in MDA-MB-231T and COLO 205 cells that overexpress Cdc7. In vivo, XL413 inhibits MCM2 phosphorylation (ED50 = <3 mg/kg) and reduces tumor growth in a COLO 205 mouse xenograft model when administered orally at doses of 10, 30, and 100 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Koltun, E.S., Tsuhako, A.L., Brown, D.S., et alDiscovery of XL413, a potent and selective CDC7 inhibitor. Bioorg. Med. Chem. Lett. 22(11), 3727-3731 (2012).