Buparlisib free base · Synonyms: BKM-120

Buparlisib is a pan-class I PI3K inhibitor.

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

Target PI3K Apoptosis

Research area Cancer

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Data Sheet SDS COA

Buparlisib structure

CAS No.: 944396-07-0

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 440.00	BP-02464-500mg	In stock	Get quote
1 g	USD 700.00	BP-02464-1g	In stock	Get quote
2 g	USD 11,125.00	BP-02464-2g	In stock	Get quote
3 g	USD 1,350.00	BP-02464-3g	In stock	Get quote
5 g	USD 1,800.00	BP-02464-5g	In stock	Get quote
10 g	USD 2,880.00	BP-02464-10g	In stock	Get quote

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Description

Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with blood-brain barrier permeability. Buparlisib has IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively .

Biological activity

In Vitro Buparlisib (NVP-BKM120) exhibits activity of 50–300 nM against class I PI3K (including the most common p110α mutant). In addition, NVP-BKM120 shows lower potency against class III and IV PI3K, with biochemical activities of 2, 5, >5 and >25 μM observed, respectively, for the inhibition of VPS34, mTOR, DNAPK and PI4K[1]. Buparlisib (≥10 μM, 24 h) induces apoptosis in multiple myeloma (MM) cells in a dose- and time-dependent manner[1]. Buparlisib (10 μM, 24 h) causes dose-dependent growth inhibition in all tested MM cell lines, with IC50 values ??between 1 and 10 μM for ARP-1, ARK, and MM.1R, while the IC50 value for MM.1S was <1 μM and for U266 it was between 10 and 100 μM[2]. In Vivo In A2780 xenograft tumors, oral dosing of Buparlisib (NVP-BKM120) at 3, 10, 30, 60, and 100 mg/kg results in a dose dependent modulation of pAKTSer473. Partial inhibition of pAKTSer473 is observed at 3 and 10 mg/kg, and near complete inhibition is observed at doses of 30, 60, or 100 mg/kg, respectively. Inhibition of pAKT (normalized to total AKT) tracked well with both plasma and tumor drug exposure[1]. Mice receiving Buparlisib (NVP-BKM120) (5 μM per kg per day for 15 days) treatment has significantly smaller tumor burdens as compare with control mice, which are measured as tumor volume (P<0.05) and level of circulating human kappa chain. In addition, NVP-BKM120 treatment significantly prolongs the survival of tumor-bearing mice (P<0.05)[2]. Buparlisib has an excellent brain penetration that is unaffected by efflux transporters at the blood-brain barrier[5].

Identifiers

SMILES: NC1=NC=C(C2=NC(=NC(=C2)N2CCOCC2)N2CCOCC2)C(=C1)C(F)(F)F
InChIKey: CWHUFRVAEUJCEF-UHFFFAOYSA-N

Specifications

MW (average): 410.3935
Formula: C₁₈H₂₁F₃N₆O₂
CAS No.: 944396-07-0
Physical state: Solid
Color: White to off-white
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/H2O

Documents

References

[1].Burger MT, et al. Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer. ACS Med Chem Lett. 2011 Aug 26;2(10):774-9.

[2].Zheng Y, et al. Novel phosphatidylinositol 3-kinase inhibitor NVP-BKM120 induces apoptosis in myeloma cells and shows synergistic anti-myeloma activity. J Mol Med (Berl). 2012 Jun;90(6):695-706.

[3]. Ni J, et al. Combination inhibition of PI3K and mTORC1 yields durable remissions in mice bearing orthotopic patient-derived xenografts of HER2-positive breast cancer brain metastases. Nat Med. 2016 Jul;22(7):723-6.

[4].Liu H, et al. Identifying and Targeting Sporadic Oncogenic Genetic Aberrations in Mouse Models of Triple Negative Breast Cancer. Cancer Discov. 2018 Mar;8(3):354-369.

[5]. de Gooijer MC, et al. Buparlisib is a brain penetrable pan-PI3K inhibitor. Sci Rep. 2018 Jul 17;8(1):10784.

Same target

Search PI3K

Same research area

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