Chengdu Henghui Pharmaceutical Co., Ltd.(expird)
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supplier - 8th
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Business Type:Lab/Research institutions
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Country: 
China (Mainland)
Business Type:Lab/Research institutions
We are a CRO company, and our Research and Development team is consisted of PhDs and Masters in chemistry and pharmacy.
We are committed to protect our customer’s privacy with the highest level of ethical standard. Our dedicated team will follow up on every order and provide instant feedback on the status to our customer.
We stand behind our product by providing a complete QA report. The test data of customer order can be provided upon request.
We make our efforts to offer customer innovative, customized, high-quality service.
Our custom manufacturing encompasses everything from pharmaceutical intermediates to API.
| XL147(SAR245408; pilaralisib) is a potent, orally bioavailable inhibitor of the class I PI3K family of lipid kinases with IC50 values of 39 nM/383 nM/36 nM/23 nM for PI3Kα/β/δ/γ, respectively; less potent to PI3Kβ. IC50 Value:39 nM (PI3Kα); 383 nM (PI3Kβ); 36 nM (PI3Kδ); 23 nM(PI3Kγ)[1] Target: in vitro: XL147 binds in an ATP-competitive and reversible manner, yet is highly selective against a panel of >130 human protein kinases. In cellular assays, XL147 antagonizes the production of the second messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) resulting in inhibition of phosphorylation of several downstream effectors of PI3K including Akt, ribosomal S6 kinase, and ribosomal S6 protein. Compared with XL147 alone, the combination exhibited a superior antitumor effect against trastuzumab-resistant tumor xenografts. Furthermore, treatment with XL147 and trastuzumab reduced the cancer stem-cell (CSC) fraction within trastuzumab-resistant cells both in vitro and in vivo. in vivo: SAR245408 induced significant differences in EFS distribution compared to control in 29 of 37 (79%) of solid tumor xenografts and in two of seven (29%) ALL. Xenografts. SAR245408 induced tumor growth inhibition meeting criteria for intermediate EFS T/C activity in 4 of 37 (11%) solid tumor xenografts. Toxicity: In vitro SAR245408 demonstrated cytotoxic activity, with a median relative IC50 value of 10.9 μM (range 2.7-24.5 μM)[4]. Clinical trial: Open-label Treatment Extension Study With SAR-245408 or SAR-245409 as a Monotherapy or as a Combination Regimen. Phase 1/Phase 2 |