GDC-0084(CAS#1382979-44-3)

Chemical Property:

Molecular Formula	C18H22N8O2
Molar Mass	382.42
Density	1.60±0.1 g/cm3(Predicted)
Solubility	DMSO: 6 mg/mL (Need ultrasonic)
pKa	2.62±0.40(Predicted)
Storage Condition	-20℃
Use	Paxalisib (GDC-0084) is a PI3K and mTOR inhibitor that can penetrate the blood-brain barrier. It inhibits PI3Kα,PI3Kβ,PI3Kδ,PI3Kγ and mTOR with Ki values of 2 nM,46 nM,3 nM,10 nM and 70 nM respectively.
In vitro study	In microsomal and stem cell cultures, GDC-0084 has good human metabolic stability and can inhibit the key signal pAKT in the PI3K pathway in normal brain tissue. GDC-0084 inhibit the proliferation of a variety of glioma cells, the IC50 range is 0.3-1.1 μm. The binding rate of GDC-0084 to plasma protein is relatively low, and the free fraction in CD-1 mouse plasma is 29.5±2.7(%,n = 3,5 μm), the binding rate to brain tissue was higher in CD-1 mice, with a free fraction of 6.7%(± 1; n = 3).
In vivo study	In the mouse brain, GDC-0084 significantly inhibited the PI3K signaling pathway, resulting in up to 90% inhibition of pAkt signaling. GDC-0084 inhibited tumor growth by 70% and 40% in U87 and GS2 orthotopic xenograft models, respectively. Its widespread distribution in brain and intracranial tumors makes it a very effective inhibitor of the PI3K signaling pathway. At present, the efficacy of GDC-0084 is being evaluated in clinical patients, and the tolerated dose of exposure is consistent with the effective dose in mouse models.

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GDC-0084(CAS#1382979-44-3)

Mechanism of action: It is a small molecule inhibitor of the PI3K, AKT, and mTOR pathways, thereby inhibiting tumor proliferation by targeting key growth signaling pathways in cancer cells.
Clinical use: Mainly used in patients with glioblastoma with newly diagnosed, non-methylated MGMT who have completed initial radiation therapy with temozolomide. In August 2020, the U.S. Food and Drug Administration (FDA) granted fast-track designation to paxalisib for the treatment of these patients. Based on the results of the Phase 2 study, paxalisib has positive results in terms of safety and efficacy as a first-line treatment for patients with newly diagnosed glioblastoma. In the intention-to-treat population, patients treated with paxalisib had better median overall survival and median progression-free survival than those treated with temozolomide (historical data).
Adverse reactions: including hyperglycemia, oral mucositis and rash.
GDC-0084 has shown some potential in the treatment of glioblastoma, but more clinical trials are still needed to further validate its efficacy and safety.

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