GDC0980 free base · Synonyms: GDC-0980 | GNE 390 | RG 7422

Apitolisib is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase inhibitor.

For research use only. Not for human or veterinary use.

Target PI3K mTOR Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

GDC0980 structure

CAS No.: 1032754-93-0

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 420.00	BP-02462-100mg	In stock	Get quote
250 mg	USD 830.00	BP-02462-250mg	In stock	Get quote
500 mg	USD 1,320.00	BP-02462-500mg	In stock	Get quote
1 g	USD 2,120.00	BP-02462-1g	In stock	Get quote
2 g	USD 3,320.00	BP-02462-2g	In stock	Get quote
3 g	USD 4,060.00	BP-02462-3g	In stock	Get quote
5 g	Inquire	BP-02462-5g	In stock	Inquire

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Description

Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a?Ki?of 17 nM for mTOR.

Biological activity

In Vitro Apitolisib (GDC-0980) is remarkably selective for several other members of the closely related PIKK family kinases: C2alpha IC50=1300 nM; C2beta IC50=7 94 nM; VPS34 IC50=2000 nM; PI4Kalpha >10 μM; PI4Kbeta >10 μM; DNA-PK Kiapp=623 nM, respectively[1]. A recent study shows that Apitolisib (GDC-0980) reduces cancer cell viability by inhibiting cell-cycle procession and inducing apoptosis with most potency in prostate (IC50 < 200 nM 50%), <500 nM 100%), breast (IC50 <200 nM 37%, <500 nM 78%) and NSCLC lines (IC50 <200 nM 29%, <500 nM 88%) and less potency in pancreatic (IC50 <200 nM 13%, <500 nM 67%) and melanoma cell lines (IC50 <200 nM 0%, <500 nM 33%). In Vivo Apitolisib (GDC-0980) (1 mg/kg, p.o.) demonstrats significant efficacy in mouse xenografts and is currently in phase I clinical trials for cancer. Clearance and PPB are low, and Apitolisib (GDC-0980) shows dose-proportional exposure from 5 mg/kg dosed in PEG to 50 mg/kg dosed in suspension in MCT, a finding attributed partially to the compound’s good solubility[1]. Apitolisib (GDC-0980) (5 mg/kg, p.o.) results in greater than 50% TGI in 15 of the 20 xenograft models. The difference in tumor response to Apitolisib (GDC-0980) treatment correlates with the duration of knockdown of pAkt/tAkt.

Identifiers

SMILES: C[C@H](O)C(=O)N1CCN(CC2=C(C)C3=NC(=NC(N4CCOCC4)=C3S2)C2=CN=C(N)N=C2)CC1
InChIKey: YOVVNQKCSKSHKT-HNNXBMFYSA-N

Specifications

MW (average): 498.6010
Formula: C₂₃H₃₀N₈O₃S
CAS No.: 1032754-93-0
Physical state: Solid
Color: White to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 year;

Solubility

Soluble in DMSO

Documents

References

[1].Sutherlin DP, et al. Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. J Med Chem, 2011, 54(21), 7579-7587.

[2].Wallin JJ, et al. GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway. Mol Cancer Ther, 2011, 10(12), 2426-2436.

Same target

Search PI3K

Same research area

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