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CH5132799

Catalog No.
B2183
Class I PI3K inhibitor
Grouped product items
SizePriceStock Qty
5mg
$170.00
Ship with 10-15 days
10mg
$274.00
Ship with 10-15 days
50mg
$718.00
Ship with 10-15 days
100mg
$1,155.00
Ship with 10-15 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

CH5132799 is an inhibitor of class I phosphatidylinositol 3-kinase (PI3K) with IC50 value of 14nM against PI3Kα [1].

CH5132799 shows inhibitory effect on class I PI3K with IC50 values of 0.014μM, 0.12μM, 0.5μM and 0.036μM against PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. PI3Kα is especially sensitive to CH5132799. CH5132799 is a selective inhibitor. It shows less effect on class II PI3Ks, class III PI3K and mTOR. For other 26 protein kinases, CH5132799 nearly has no inhibition with IC50 value of > 10μM. CH5132799 is found to have potent antitumor activity. It exerts IC50 values of 0.2μM, 0.032μM, 0.056μM and 0.12μM in HCT116, KPL-4, T-47D and SK-OV-3 cell lines, respectively. Moreover, CH5132799 is oral available in animal models. Treatment of CH5132799 shows strong tumor regression at dose of 12.5 mg/kg in mice bearing human breast cancer xenografts [1].

References:
[1] Ohwada J, Ebiike H, Kawada H, et al. Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. Bioorganic & medicinal chemistry letters, 2011, 21(6): 1767-1772.

Chemical Properties

StorageStore at -20°C
M.Wt377.42
Cas No.1007207-67-1
FormulaC15H19N7O3S
SolubilitySoluble in DMSO
Chemical Name5-(7-methylsulfonyl-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine
SDFDownload SDF
Canonical SMILESCS(=O)(=O)N1CCC2=C(N=C(N=C21)N3CCOCC3)C4=CN=C(N=C4)N
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Biological Activity

Description CH5132799 is an inhibitor of class I PI3Ks.
Targets PI3Kα PI3Kγ PI3Kβ PI3Kδ mTOR  
IC50 14 nM 36 nM 0.12 μM 0.50 μM 1.6 μM  

Quality Control

Quality Control & MSDS

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Chemical structure

CH5132799