Buparlisib (Synonyms: 布帕尼西; BKM120; NVP-BKM120)

目錄號: HY-70063 純度: 99.82%: FAQs
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Buparlisib (BKM120; NVP-BKM120) 是一種 pan-class I PI3K 抑制劑，作用于 p110α/p110β/p110δ/p110γ，IC₅₀ 分別為 52 nM/166 nM/116 nM/262 nM。

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Buparlisib Chemical Structure

CAS No. : 944396-07-0

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規(guī)格	價格	是否有貨
10 mM * 1 mL in DMSO	￥715	In-stock
5 mg	￥650	In-stock
10 mg	￥920	In-stock
50 mg	￥1850	In-stock
100 mg	￥2780	In-stock
200 mg	￥4200	In-stock
500 mg	現(xiàn)貨	詢價
1 g		詢價
5 g		詢價

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Other Forms of Buparlisib:

Buparlisib Hydrochloride In-stock

MCE 顧客使用本產品發(fā)表的 72 篇科研文獻

•Nature. 2024 Sep;633(8031):895-904. [Abstract]
•Nature. 2022 Dec;612(7940):555-563. [Abstract]
•Nature. 2018 Aug;560(7719):499-503. [Abstract]
•Nat Med. 2016 Jul;22(7):723-6. [Abstract]
•Cancer Discov. 2020 Aug;10(8):1226-1239. [Abstract]
•Cancer Discov. 2019 Sep;9(9):1306-1323. [Abstract]

•Nat Biomed Eng. 2018 Aug;2(8):578-588. [Abstract]
•Cancer Discov. 2018 Mar;8(3):354-369. [Abstract]
•Nat Cancer. 2024 Jul 11. [Abstract]
•Sci Transl Med. 2023 Feb 22;15(684):eade1857. [Abstract]
•J Exp Med. 2023 Nov 6;220(11):e20211743. [Abstract]
•Cancer Commun (Lond). 2022 Feb 18. [Abstract]
•Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. [Abstract]
•Nat Commun. 2022 Sep 29;13(1):5723. [Abstract]
•Cancer Res. 2022 Jul 27;CAN-22-0042. [Abstract]
•Sci Adv. 2022 Jan 21;8(3):eabh2635. [Abstract]
•Autophagy. 2022 Jul;18(7):1551-1571. [Abstract]
•Nat Commun. 2021 Jun 8;12(1):3444. [Abstract]
•Nat Commun. 2020 May 19;11(1):2487. [Abstract]
•Diabetologia. 2021 Feb 11. [Abstract]
•Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]
•Cell Commun Signal. 2019 May 15;17(1):44. [Abstract]
•ACS Appl Mater Interfaces. 2019 Apr 3;11(13):12342-12356. [Abstract]
•Cancer Lett. 2019 Jan;440-441:54-63. [Abstract]
•Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]
•Proc Natl Acad Sci U S A. 2018 Oct 9;115(41):E9570-E9579. [Abstract]
•J Transl Med. 2024 Nov 7;22(1):1004. [Abstract]
•Biomed Pharmacother. 2024 Oct 16:180:117569. [Abstract]
•Cell Rep. 2024 Apr 23;43(5):114132. [Abstract]
•J Cell Biol. 2023 Sep 4;222(9):e202208150. [Abstract]
•Oncogene. 2022 Jan 20. [Abstract]
•J Cell Biol. 2020 Dec 7;219(12):e202001031. [Abstract]
•Cell Rep. 2020 Sep 29;32(13):108196. [Abstract]
•Sci Signal. 2019 May 28;12(583). pii: eaaw9450. [Abstract]
•Oncoimmunology. 2019 Mar 16;8(5):e1581556. [Abstract]
•Oncogene. 2016 Jul 7;35(27):3607-12. [Abstract]
•Cancers (Basel). 2024 Aug 7;16(16):2785. [Abstract]
•Cancer Immunol Immunother. 2024 May 7;73(7):122. [Abstract]
•Mol Carcinog. 2024 Apr 17
•World J Gastroenterol. 2023 Oct 28.
•Endocrinology. 2023 Sep 13;bqad135. [Abstract]
•Eur J Pharmacol. 2023 May 2;175747. [Abstract]
•Cancers (Basel). 2022, 14(22), 5481
•Biomedicines. 2022, 10(8), 1988.
•Mol Carcinog. 2022 Apr 13. [Abstract]
•J Clin Endocrinol Metab. 2021 Jan 1;106(1):e232-e246. [Abstract]
•Molecules. 2020 Apr 23;25(8):1980. [Abstract]
•Cancer Cell Int. 2020 Mar 18;20:86. [Abstract]
•Hepatol Commun. 2019 Feb 5;3(3):423-436. [Abstract]
•Sci Rep. 2019 Jan 30;9(1):978. [Abstract]
•Clin Med Insights Oncol. 2024 Oct 16:18:11795549241285387. [Abstract]
•BMC Anesthesiol. 2021 Aug 30;21(1):210. [Abstract]
•In Vitro Cell Dev Biol Anim. 2021 May 5. [Abstract]
•Am J Transl Res. 2019 Sep 15;11(9):6055-6065. [Abstract]
•Brain Behav. 2018 Nov;8(11):e01123. [Abstract]
•PLoS One. 2018 Jul 5;13(7):e0200014. [Abstract]
•Prostate. 2018 Feb;78(3):166-177. [Abstract]
•PLoS One. 2016 Jan 28;11(1):e0147682. [Abstract]
•Anticancer Res. 2018 Jun;38(6):3375-3385. [Abstract]
•bioRxiv. 2024 Dec 10:2024.12.09.627542. [Abstract]
•Patent. US20210236501A1.
•bioRxiv. 2022 Aug 02.
•bioRxiv. 2023 Aug 13.
•bioRxiv. 2023 Jul 24.
•University of Gothenburg. 2023 Jun 27.
•Research Square Print. 10 Jan 2023.
•Research Square Print. November 7th, 2022
•Journal of the Endocrine Society. 2021 Jun 1.
•Programa de Doctorado en Biomedicina. 2020 Sep.
•Cold Spring Harb Mol Case Stud. 2020 Jun 12;6(3):a004853. [Abstract]
•Patent. US20160215053A1.
•Harvard Medical School LINCS LIBRARY

: Buparlisib purchased from MCE. Usage Cited in: Cancer Lett. 2019 Jan;440-441:54-63. [Abstract]; The cells are transfected with either the negative control (siNC) or BTF3 siRNA for 12 hours followed by BKM-120 or AZD-6482 treatment for 48 hours. The protein abundance is determined by an immunoblotting analysis.

: Buparlisib purchased from MCE. Usage Cited in: Brain Behav. 2018 Nov;8(11):e01123. [Abstract]; The effect of BKM120 on AKT phosphorylation is examined by Western blot.

: Buparlisib purchased from MCE. Usage Cited in: PLoS One. 2018 Jul 5;13(7):e0200014. [Abstract]; Representative immunoblots of control and NHA^RAS treated with Buparlisib for 24 h.

: Buparlisib purchased from MCE. Usage Cited in: Prostate. 2018 Feb;78(3):166-177. [Abstract]; Western blot analysis of p-AKT (Ser473) in stable cell lines (Vector-DU145 and GOLM1-DU145) treated with 200 nM, 500 nM or 1 μM BKM120.

: Buparlisib purchased from MCE. Usage Cited in: Nat Med. 2016 Jul;22(7):723-6. [Abstract]; Selective response of HER2-positive PDX DF-BM355 to the combination of BKM120/RAD001. Western blot analysis of lysates from vehicle-treated or BKM120-treated DF-BM355 in vivo.

: Buparlisib purchased from MCE. Usage Cited in: Oncogene. 2016 Jul 7;35(27):3607-12. [Abstract]; (A) Immunoblot analyses in HCC1569 cells treated with BYL719, KIN193 (MedChemexpress) or BKM120 (μM). (B, C) Immunoblot analyses in BT474 and BT474-shPTEN cells treated as indicated in (A).

Buparlisib 相關產品

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

生物活性
實驗參考方法
純度 & 產品資料
參考文獻

生物活性

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

IC₅₀ & Target^[1]

p110α

52 nM (IC₅₀)

p110α-H1047R

58 nM (IC₅₀)

p110α-E545K

99 nM (IC₅₀)

p110δ

116 nM (IC₅₀)

p110β

166 nM (IC₅₀)

p110γ

262 nM (IC₅₀)

Vps34

2.4 μM (IC₅₀)

mTOR

4.6 μM (IC₅₀)

細胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A2780	EC₅₀	0.055 μM Compound: 15, NVP-BKM120	Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human A2780 cells after 1 hr Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human A2780 cells after 1 hr	[PMID: 24900266]
A2780	EC₅₀	0.074 μM Compound: 15, NVP-BKM120	Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human A2780 cells after 1 hr Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human A2780 cells after 1 hr	[PMID: 24900266]
A2780	EC₅₀	0.52 μM Compound: 15, NVP-BKM120	Antiproliferative activity against human A2780 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human A2780 cells after 3 days by CellTiter-Glo assay	[PMID: 24900266]
A2780	GI₅₀	0.635 nM Compound: 15, NVP-BKM120	Cytotoxicity against PTEN-deficient human A2780 cells after 3 days by CellTiterGlo assay Cytotoxicity against PTEN-deficient human A2780 cells after 3 days by CellTiterGlo assay	[PMID: 24900266]
A-431	IC₅₀	1.03 μM Compound: 5a	Antiproliferative activity against human A431 cells after 72 hrs by CCK8 assay Antiproliferative activity against human A431 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
A549	IC₅₀	1.51 μM Compound: 5a	Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
A549	IC₅₀	2.07 μM Compound: BKM120	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 25765909]
Bel-7402	IC₅₀	1.92 μM Compound: 5a	Antiproliferative activity against human Bel7402 cells after 72 hrs by CCK8 assay Antiproliferative activity against human Bel7402 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
Bel-7402	IC₅₀	13 μM Compound: 4; BKM120	Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay	[PMID: 31117517]
BGC-823	IC₅₀	1.43 μM Compound: 5a	Antiproliferative activity against human BGC823 cells after 72 hrs by CCK8 assay Antiproliferative activity against human BGC823 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
Capan-2	IC₅₀	42 μM Compound: 4; BKM120	Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay	[PMID: 31117517]
D283 Med	IC₅₀	0.279 μM Compound: BKM120	Cytotoxicity against human D283 Med cells assessed as reduction in cell viability incubated for 48 hrs by Cell TiterGlo luminescent assay Cytotoxicity against human D283 Med cells assessed as reduction in cell viability incubated for 48 hrs by Cell TiterGlo luminescent assay	[PMID: 33636537]
Daoy	IC₅₀	0.279 μM Compound: BKM120	Cytotoxicity against human Daoy cells assessed as reduction in cell viability incubated for 48 hrs by Cell TiterGlo luminescent assay Cytotoxicity against human Daoy cells assessed as reduction in cell viability incubated for 48 hrs by Cell TiterGlo luminescent assay	[PMID: 33636537]
DU-145	EC₅₀	0.073 μM Compound: 15, NVP-BKM120	Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human DU145 cells harboring LKB1 mutation after 1 hr Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human DU145 cells harboring LKB1 mutation after 1 hr	[PMID: 24900266]
DU-145	IC₅₀	0.91 μM Compound: 5a	Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
DU-145	IC₅₀	45 μM Compound: 4; BKM120	Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay	[PMID: 31117517]
HCT-116	IC₅₀	0.48 μM Compound: BKM120	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 25765909]
HCT-116	IC₅₀	1.3 μM Compound: 4; BKM120	Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay	[PMID: 31117517]
HCT-8	IC₅₀	1.7 μM Compound: 4; BKM120	Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay	[PMID: 31117517]
HeLa	IC₅₀	1.17 μM Compound: 5a	Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay	[PMID: 27427973]
HeLa	IC₅₀	4.34 μM Compound: BKM120	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay	[PMID: 25765909]
HepG2	IC₅₀	3.2 μM Compound: 4; BKM120	Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay	[PMID: 31117517]
HGC-27	IC₅₀	0.99 μM Compound: 4; BKM120	Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay	[PMID: 31117517]
HL-60	IC₅₀	1.51 μM Compound: BKM120	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 36272186]
HT-1080	IC₅₀	2.08 μM Compound: 5a	Antiproliferative activity against human HT1080 cells after 72 hrs by CCK8 assay Antiproliferative activity against human HT1080 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
Huh-7	IC₅₀	1.51 μM Compound: 5a	Antiproliferative activity against human HuH7 cells after 72 hrs by CCK8 assay Antiproliferative activity against human HuH7 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
Huh-7	IC₅₀	2 μM Compound: 4; BKM120	Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay	[PMID: 31117517]
HUVEC	IC₅₀	0.886 μM Compound: NVP-BKM120; BKM	Cytotoxicity against HUVEC after 72 hrs by MTT assay Cytotoxicity against HUVEC after 72 hrs by MTT assay	[PMID: 30034607]
K562	IC₅₀	0.73 μM Compound: BKM120	Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 36272186]
K562	IC₅₀	1.1 μM Compound: 5a	Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
K562	IC₅₀	7.9 μM Compound: 4; BKM120	Antiproliferative activity against human K562 cells after 96 hrs by MTT assay Antiproliferative activity against human K562 cells after 96 hrs by MTT assay	[PMID: 31117517]
MCF7	EC₅₀	< 0.1 μM Compound: 15, NVP-BKM120	Inhibition of PI3Kalpha E545K mutant-mediated AKT Ser473 phosphorylation in human MCF7 cells after 1 hr Inhibition of PI3Kalpha E545K mutant-mediated AKT Ser473 phosphorylation in human MCF7 cells after 1 hr	[PMID: 24900266]
MCF7	IC₅₀	0.206 μM Compound: NVP-BKM120; BKM	Antiproliferative activity against human MCF7 cells harboring PIK3CA E545K mutant after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells harboring PIK3CA E545K mutant after 72 hrs by MTT assay	[PMID: 30034607]
MCF7	IC₅₀	1 μM Compound: BKM120	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 25765909]
MCF7	IC₅₀	1.5 μM Compound: 5a	Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
MCF7	IC₅₀	11.05 μM Compound: Buparlisib	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 29107429]
MCF7	IC₅₀	5.7 μM Compound: 4; BKM120	Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay	[PMID: 31117517]
MDA-MB-231	IC₅₀	1.88 μM Compound: Buparlisib	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 29107429]
MDA-MB-453	IC₅₀	0.37 μM Compound: 4; BKM120	Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay	[PMID: 31117517]
MDA-MB-468	IC₅₀	3.97 μM Compound: BKM120	Antiproliferative activity against human MDA-MB-468 cells measured after 7 days by Celltiter-glo assay Antiproliferative activity against human MDA-MB-468 cells measured after 7 days by Celltiter-glo assay	[PMID: 33309164]
MOLT-4	IC₅₀	0.8 μM Compound: 5a	Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
MV4-11	IC₅₀	0.73 μM Compound: BKM120	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 36272186]
NCI-H1299	IC₅₀	3.6 μM Compound: 4; BKM120	Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay	[PMID: 31117517]
NCI-H460	IC₅₀	3.2 μM Compound: 4; BKM120	Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay	[PMID: 31117517]
NCI-N87	IC₅₀	0.66 μM Compound: 5a	Antiproliferative activity against human NCI-N87 cells after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-N87 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
PANC-1	IC₅₀	1.83 μM Compound: 5a	Antiproliferative activity against human PANC1 cells after 72 hrs by CCK8 assay Antiproliferative activity against human PANC1 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
PC-3	IC₅₀	5.34 μM Compound: Buparlisib	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 29107429]
SGC-7901	IC₅₀	1.24 μM Compound: 5a	Antiproliferative activity against human SGC7901 cells after 72 hrs by CCK8 assay Antiproliferative activity against human SGC7901 cells after 72 hrs by CCK8 assay	[PMID: 27427973]
SW1990	IC₅₀	1.3 μM Compound: 4; BKM120	Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay	[PMID: 31117517]
T47D	IC₅₀	0.286 μM Compound: NVP-BKM120; BKM	Antiproliferative activity against human T47D cells harboring PI3KCA H1047R mutant after 72 hrs by MTT assay Antiproliferative activity against human T47D cells harboring PI3KCA H1047R mutant after 72 hrs by MTT assay	[PMID: 30034607]
T47D	IC₅₀	6.92 μM Compound: Buparlisib	Cytotoxicity against human T47D cells after 72 hrs by MTT assay Cytotoxicity against human T47D cells after 72 hrs by MTT assay	[PMID: 29107429]
THP-1	IC₅₀	12 μM Compound: 4; BKM120	Antiproliferative activity against human THP1 cells after 96 hrs by MTT assay Antiproliferative activity against human THP1 cells after 96 hrs by MTT assay	[PMID: 31117517]
U-87MG ATCC	EC₅₀	0.13 μM Compound: 15, NVP-BKM120	Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human U87MG cells after 1 hr Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human U87MG cells after 1 hr	[PMID: 24900266]
U-87MG ATCC	IC₅₀	1.64 μM Compound: BKM120	Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay	[PMID: 25765909]
U-87MG ATCC	IC₅₀	4.8 μM Compound: 4; BKM120	Antiproliferative activity against human U87 cells after 96 hrs by MTT assay Antiproliferative activity against human U87 cells after 96 hrs by MTT assay	[PMID: 31117517]
U-937	IC₅₀	0.58 μM Compound: 5a	Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay	[PMID: 27427973]

體外研究
(In Vitro)

Buparlisib (NVP-BKM120) 對 I 類 PI3K（包括最常見的 p110α 突變體）表現(xiàn)出 50-300 nM 的活性。此外，NVP-BKM120 對 III 類和 IV 類 PI3K 表現(xiàn)出較低的效力，其中分別觀察到 2、5、>5 和 >25 μM 的生化活性，用于抑制 VPS34、mTOR、DNAPK 和 PI4K^[1]。Buparlisib (NVP-BKM120) 以劑量和時間依賴性方式誘導多發(fā)性骨髓瘤 (MM) 細胞凋亡。濃度≥10 μM 的 Buparlisib (NVP-BKM120) 在 24 小時后在所有測試的 MM 細胞系中誘導顯著細胞凋亡（與對照組相比，P<0.05）。因此，如無特別說明，以下實驗均選擇 10 μM Buparlisib (NVP-BKM120) 和 24 小時治療。Buparlisib (NVP-BKM120) 治療會導致所有測試的 MM 細胞系出現(xiàn)劑量依賴性生長抑制。Buparlisib (NVP-BKM120) IC₅₀ 因測試的 MM 細胞而異。在 24 小時治療中，ARP-1、ARK 和 MM.1R 的 IC₅₀ 在 1 至 10 μM 之間，而 MM.1S 的 IC₅₀ 為 <1 μM，U266 的 IC₅₀ 在 10 至 100 μM 之間?？傊?，NVP-BKM120 治療會導致 MM 細胞生長抑制和凋亡，且呈劑量和時間依賴性^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

體內研究
(In Vivo)

在 A2780 異種移植腫瘤中，口服 3、10、30、60 和 100 mg/kg Buparlisib (NVP-BKM120) 會導致 pAKT^Ser473 發(fā)生劑量依賴性調節(jié)。在 3 和 10 mg/kg 劑量下觀察到 pAKT^Ser473 的部分抑制，在 30、60 或 100 mg/kg 劑量下觀察到接近完全的抑制。pAKT 的抑制（以總 AKT 為標準）與血漿和腫瘤藥物暴露量均有很好的跟蹤^[1]。接受 Buparlisib (NVP-BKM120)（每天每公斤 5 μM，持續(xù) 15 天）治療的小鼠的腫瘤負擔明顯小于對照小鼠，以腫瘤體積（P<0.05）和循環(huán)人類 κ 鏈水平（P<0.05）來衡量。此外，NVP-BKM120 治療顯著延長了荷瘤小鼠的生存期（P<0.05）^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

410.39

Formula

C₁₈H₂₁F₃N₆O₂

CAS 號

944396-07-0

性狀

固體

顏色

White to off-white

中文名稱

布帕尼西

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性數(shù)據

細胞實驗：

DMSO 中的溶解度 : 100 mg/mL (243.67 mM; 超聲助溶; 吸濕的 DMSO 對產品的溶解度有顯著影響，請使用新開封的 DMSO)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲備液

濃度溶劑體積質量	1 mg	5 mg	10 mg

1 mM	2.4367 mL	12.1835 mL	24.3671 mL
5 mM	0.4873 mL	2.4367 mL	4.8734 mL
10 mM	0.2437 mL	1.2184 mL	2.4367 mL

查看完整儲備液配制表

* 請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內使用， -20°C儲存時，請在1年內使用。

摩爾計算器
稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動物實驗：

請根據您的實驗動物和給藥方式選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結果的可靠性，澄清的儲備液可以根據儲存條件，適當保存；體內實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

方案一

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.09 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.09 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案三

請依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.09 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。
方案四

請依序添加每種溶劑： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (6.09 mM); 澄清溶液
方案五

請依序添加每種溶劑： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.09 mM); 澄清溶液

以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內盡快用完。以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

方案一

請依序添加每種溶劑： 50% PEG300 50% Saline
Solubility: 2.08 mg/mL (5.07 mM); 懸濁液; 超聲助溶

動物溶解方案計算器

請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

每只動物的給藥體積

μL

動物數(shù)量

只

由于實驗過程有損耗，建議您多配一只動物的量

請輸入您的動物體內配方組成：

DMSO +

Tween-80 +

Saline

如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網站選購。，Tween 80，均可在 MCE 網站選購。

計算結果

工作液所需濃度 : mg/mL

儲備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲備液濃度超過該產品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術支持聯(lián)系。

動物實驗體內工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。

請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產品資料

純度: 99.90%

選擇批次：

Data Sheet (657 KB) SDS (393 KB)

COA (288 KB) HNMR (192 KB) LCMS (122 KB)

產品使用指南 (1538 KB)

參考文獻

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Cell Assay ^[1]	A2780 cells are cultured in DMEM supplemented with 10% FBS. L-glutamine, sodium pyruvate, and antibiotics. Cells are plated in the same medium at a density of 1000 cells per well, 100 uL per well into black-walled-clear-bottom plates and incubated for 3-5 hours. Buparlisib (NVP-BKM120) supplied in DMSO (20 mM) are diluted further into DMSO (7.5 uL of 20 mM Buparlisib (NVP-BKM120) in 22.5 uL DMSO. Mix well, transfer 10 uL to 20 uL DMSO, repeat until 9 concentrations have been made). The diluted Buparlisib (NVP-BKM120) solution (2 uL), is then added to cell medium (500 uL) cell medium. Equal volumes of this solution (100 uL) are added to the cells in 96 well plates and incubated at 37oC for 3 days and developed using Cell Titer Glo. Inhibition of cell proliferation is determined by luminescence read using Trilux^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[2] Six- to eight-week-old female severe combined immunodeficiency (SCID) mice are used. SCID mice are subcutaneously inoculated in the right flank with 1 million ARP-1 or MM.1S cells suspended in 50 μL phosphate-buffered saline (PBS). After palpable tumor developed (tumor diameter ≥5 mm), mice are treated with intraperitoneal injection of DMSO/PBS or Buparlisib (NVP-BKM120) (5 μM per kg per day) for 15 days. Tumor sizes are measured every 5 days, and blood samples are collected at the same period. Tumor burdens are evaluated by measuring tumor size and detecting circulating human kappa chain or lambda chain. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻	[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. [Content Brief] [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. [Content Brief] [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. [Content Brief] [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. [Content Brief]

Buparlisib 相關分類

完整儲備液配制表

可選溶劑	濃度溶劑體積質量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4367 mL	12.1835 mL	24.3671 mL	60.9177 mL
	5 mM	0.4873 mL	2.4367 mL	4.8734 mL	12.1835 mL
	10 mM	0.2437 mL	1.2184 mL	2.4367 mL	6.0918 mL
	15 mM	0.1624 mL	0.8122 mL	1.6245 mL	4.0612 mL
	20 mM	0.1218 mL	0.6092 mL	1.2184 mL	3.0459 mL
	25 mM	0.0975 mL	0.4873 mL	0.9747 mL	2.4367 mL
	30 mM	0.0812 mL	0.4061 mL	0.8122 mL	2.0306 mL
	40 mM	0.0609 mL	0.3046 mL	0.6092 mL	1.5229 mL
	50 mM	0.0487 mL	0.2437 mL	0.4873 mL	1.2184 mL
	60 mM	0.0406 mL	0.2031 mL	0.4061 mL	1.0153 mL
	80 mM	0.0305 mL	0.1523 mL	0.3046 mL	0.7615 mL
	100 mM	0.0244 mL	0.1218 mL	0.2437 mL	0.6092 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Buparlisib944396-07-0BKM120 NVP-BKM120布帕尼西BKM 120BKM-120PI3KApoptosisPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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Buparlisib (Synonyms: 布帕尼西; BKM120; NVP-BKM120)

Customer Review

Other Forms of Buparlisib:

MCE 顧客使用本產品發(fā)表的 72 篇科研文獻

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純度 & 產品資料

參考文獻

摩爾計算器

稀釋計算器

Buparlisib 相關分類

完整儲備液配制表

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Buparlisib (Synonyms: 布帕尼西; BKM120; NVP-BKM120)

Customer Review

Other Forms of Buparlisib:

Buparlisib 相關抗體

MCE 顧客使用本產品發(fā)表的 72 篇科研文獻

Buparlisib 相關產品

•相關化合物庫:

•同靶點產品:

•同靶點蛋白產品:

查看 PI3K 亞型特異性產品:

生物活性

實驗參考方法

純度 & 產品資料

參考文獻

Buparlisib 相關抗體:

摩爾計算器

稀釋計算器

Buparlisib 相關分類

完整儲備液配制表

Keywords:

您最近查看的產品:

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