GSK2126458 free base · Synonyms: Omipalisib

Omipalisib is an orally active and highly selective inhibitor of PI3K.

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

Target PI3K mTOR Autophagy

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

GSK2126458 structure

CAS No.: 1086062-66-9

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 480.00	BP-02294-250mg	In stock	Get quote
500 mg	USD 750.00	BP-02294-500mg	In stock	Get quote
1 g	USD 1,220.00	BP-02294-1g	In stock	Get quote
2 g	USD 1,960.00	BP-02294-2g	In stock	Get quote
3 g	USD 2,350.00	BP-02294-3g	In stock	Get quote
5 g	USD 3,145.00	BP-02294-5g	In stock	Get quote
10 g	Inquire	BP-02294-10g	In stock	Inquire

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Description

Omipalisib (GSK2126458) is an orally active and highly selective inhibitor of PI3K with Kis of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2, respectively. Omipalisib has anti-cancer activity .

Biological activity

In Vitro Omipalisib (GSK2126458) potently inhibits the activity of common activating mutants of p110α (E542K, E545K, and H1047R) found in human cancer with Ki of 8 pM, 8 pM and 9 pM, respectively. Omipalisib causes a significant reduction in the levels of pAkt-S473 with remarkable potency in T47D and BT474 cells with IC50 of 0.41 nM and 0.18 nM, respectively. Furthermore, Omipalisib (GSK2126458) leads to a G1 cell cycle arrest and produces the inhibitory effect on cell proliferation in a large panel of cell lines, including T47D and BT474 breast cancer lines with IC50 of 3 nM and 2.4 nM, respectively[1]. The combination of Omipalisib or GSK1120212 with Omipalisib enhances cell growth inhibition and decreases S6 ribosomal protein phosphorylation in drug-resistant clones from the A375 BRAF(V600E) and the YUSIT1 BRAF(V600K) melanoma cell lines[2]. Omipalisib (GSK2126458) potentiates the antiproliferative activity of DDR1-IN-1 in colorectal cancer cell lines. In Vivo In a BT474 human tumor xenograft model, Omipalisib (GSK2126458) treatment results in a dose-dependent reduction in pAkt-S473 levels, and exhibits dose-dependent tumor growth inhibition at a low dose of 300 μg/kg. Besides, Omipalisib (GSK2126458) shows low blood clearance and good oral bioavailability in four preclinical species (mouse, rat, dog, and monkey)[1].

Identifiers

SMILES: COC1=NC=C(C=C1NS(=O)(=O)C1=CC=C(F)C=C1F)C1=CC=C2N=CC=C(C3=CC=NN=C3)C2=C1
InChIKey: CGBJSGAELGCMKE-UHFFFAOYSA-N

Specifications

MW (average): 505.4960
Formula: C₂₅H₁₇F₂N₅O₃S
CAS No.: 1086062-66-9
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 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Knight SD, et al. Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin. ACS Med. Chem. Lett. 2010, 1 (1), 39-43.

[2]. Greger JG, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther. 2012 Apr;11(4):909-20.

[3]. Kim HG, et al. Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS Chem Biol. 2013 Oct 18;8(10):2145-50.

Same target

Search PI3K

Same research area

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