CH5132799
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.
Storage | Store at -20°C |
M.Wt | 377.42 |
Cas No. | 1007207-67-1 |
Formula | C15H19N7O3S |
Solubility | Soluble in DMSO |
Chemical Name | 5-(7-methylsulfonyl-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine |
SDF | Download SDF |
Canonical SMILES | CS(=O)(=O)N1CCC2=C(N=C(N=C21)N3CCOCC3)C4=CN=C(N=C4)N |
Shipping Condition | Small 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. |
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 & MSDS
- View current batch:
-
Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
