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Formula | C24H28N8O2 |
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Molecular Weight | 460.53 | CAS No. | 1282512-48-4 | |
Solubility (25°C)* | In vitro | DMSO | 92 mg/mL (199.76 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Taselisib (GDC 0032, RG7604) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ. | |||||||||||
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In vitro | GDC-0032 is an orally bioavailable, potent, and selective inhibitor of Class I PI3Kα, δ, and γ isoforms, with 30 fold less inhibition of the PI3K β isoform relative to the PI3Kα isoform. Preclinical data show that GDC-0032 has increased activity against PI3Kα isoform (PIK3CA) mutant and HER2-amplified cancer cell lines. GDC-0032 inhibits MCF7-neo/HER2 cells proliferation with IC50 of 2.5 nM. [1] |
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In vivo | GDC-0032 pharmacokinetics is approximately dose proportional and time independent with a mean t1/2 of 40 hours. The combination of GDC-0032 enhances activity resulting in tumor regressions and tumor growth delay (91% tumor growth inhibition (TGI)). In addition, the combination of GDC-0032 enhances the efficacy in vivo (102%TGI for GDC-0032). [1] |
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Features | A beta isoform-sparing PI3K inhibitor. |
Kinase Assay: |
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Animal Study: |
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AKT1 phosphorylation of cytoplasmic ME2 induces a metabolic switch to glycolysis for tumorigenesis [ Nat Commun, 2024, 15(1):686] | PubMed: 38263319 |
ERK signaling promotes resistance to TRK kinase inhibition in NTRK fusion-driven glioma mouse models [ Cell Rep, 2024, 43(10):114829] | PubMed: 39365700 |
Assessments of prostate cancer cell functions highlight differences between a pan-PI3K/mTOR inhibitor, gedatolisib, and single-node inhibitors of the PI3K/AKT/mTOR pathway [ Mol Oncol, 2024, 10.1002/1878-0261.13703] | PubMed: 39092562 |
The combination of breast cancer PDO and mini-PDX platform for drug screening and individualized treatment [ J Cell Mol Med, 2024, 28(9):e18374] | PubMed: 38722288 |
Azeliragon inhibits PAK1 and enhances the therapeutic efficacy of AKT inhibitors in pancreatic cancer [ Eur J Pharmacol, 2023, 948:175703] | PubMed: 37028543 |
Selective Inhibition of PI3K Isoforms in Brain Tumors Suppresses Tumor Growth by Increasing Radiosensitivity [ Yonsei Med J, 2023, 64(2):139-147] | PubMed: 36719022 |
Selective Inhibition of PI3K Isoforms in Brain Tumors Suppresses Tumor Growth by Increasing Radiosensitivity [ Yonsei Med J, 2023, 64(2):139-147] | PubMed: 36719022 |
PI3K drives the de novo synthesis of coenzyme A from vitamin B5 [ Nature, 2022, 608(7921):192-198] | PubMed: 35896750 |
MEK inhibition overcomes chemoimmunotherapy resistance by inducing CXCL10 in cancer cells [ Cancer Cell, 2022, S1535-6108(21)00662-0] | PubMed: 35051357 |
The Oncogenic PI3K-Induced Transcriptomic Landscape Reveals Key Functions in Splicing and Gene Expression Regulation [ Cancer Res, 2022, 82(12):2269-2280] | PubMed: 35442400 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.