Buparlisib (BKM120)

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MedKoo CAT#: 204690

CAS#: 944396-07-0 (free base)

Description: Buparlisib, also known as BKM120, is an orally bioavailable specific oral inhibitor of the pan-class I phosphatidylinositol 3-kinase (PI3K) family of lipid kinases with potential antineoplastic activity. PI3K inhibitor BKM120 specifically inhibits class I PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway in an ATP-competitive manner, thereby inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate and activation of the PI3K signaling pathway.

Chemical Structure

Buparlisib (BKM120)
CAS# 944396-07-0 (free base)

Theoretical Analysis

MedKoo Cat#: 204690
Name: Buparlisib (BKM120)
CAS#: 944396-07-0 (free base)
Chemical Formula: C18H21F3N6O2
Exact Mass: 410.16781
Molecular Weight: 410.39
Elemental Analysis: C, 52.68; H, 5.16; F, 13.89; N, 20.48; O, 7.80

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50.0g USD 9950.0 2 Weeks
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Related CAS #: 944396-07-0 (free base)   1312445-63-8 (HCl)    

Synonym: NVPBKM120; NVP BKM120; NV- BKM120; BKM120; BKM-120; BKM 120; Buparlisib.

IUPAC/Chemical Name: 5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine.


InChi Code: InChI=1S/C18H21F3N6O2/c19-18(20,21)13-9-15(22)23-11-12(13)14-10-16(26-1-5-28-6-2-26)25-17(24-14)27-3-7-29-8-4-27/h9-11H,1-8H2,(H2,22,23)


Appearance: white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: 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 Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO.

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 410.39 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Rodon J, Braña I, Siu LL, De Jonge MJ, Homji N, Mills D, Di Tomaso E, Sarr C, Trandafir L, Massacesi C, Eskens F, Bendell JC. Phase I dose-escalation and -expansion study of buparlisib (BKM120), an oral pan-Class I PI3K inhibitor, in patients with advanced solid tumors. Invest New Drugs. 2014 Mar 21. [Epub ahead of print] PubMed PMID: 24652201.

2: Ando Y, Inada-Inoue M, Mitsuma A, Yoshino T, Ohtsu A, Suenaga N, Sato M, Kakizume T, Robson M, Quadt C, Doi T. Phase I dose-escalation study of buparlisib (BKM120), an oral pan-class I PI3K inhibitor, in Japanese patients with advanced solid tumors. Cancer Sci. 2014 Mar;105(3):347-53. doi: 10.1111/cas.12350. Epub 2014 Feb 13. PubMed PMID: 24405565.

3: Liang YC, Wu HG, Xue HJ, Liu Q, Shi LL, Liu T, Wu G. Effects of PI3K inhibitor NVP-BKM120 on acquired resistance to gefitinib of human lung adenocarcinoma H1975 cells. J Huazhong Univ Sci Technolog Med Sci. 2013 Dec;33(6):845-51. doi: 10.1007/s11596-013-1209-5. Epub 2013 Dec 13. PubMed PMID: 24337846.

4: Lonetti A, Antunes IL, Chiarini F, Orsini E, Buontempo F, Ricci F, Tazzari PL, Pagliaro P, Melchionda F, Pession A, Bertaina A, Locatelli F, McCubrey JA, Barata JT, Martelli AM. Activity of the pan-class I phosphoinositide 3-kinase inhibitor NVP-BKM120 in T-cell acute lymphoblastic leukemia. Leukemia. 2013 Nov 6. doi: 10.1038/leu.2013.369. [Epub ahead of print] PubMed PMID: 24310736.

5: Geisthoff UW, Nguyen HL, Hess D. Improvement in hereditary hemorrhagic telangiectasia after treatment with the phosphoinositide 3-kinase inhibitor BKM120. Ann Hematol. 2014 Apr;93(4):703-4. doi: 10.1007/s00277-013-1845-7. Epub 2013 Jul 27. PubMed PMID: 23892886.

6: Rosich L, Saborit-Villarroya I, López-Guerra M, Xargay-Torrent S, Montraveta A, Aymerich M, Villamor N, Campo E, Pérez-Galán P, Roué G, Colomer D. The phosphatidylinositol-3-kinase inhibitor NVP-BKM120 overcomes resistance signals derived from microenvironment by regulating the Akt/FoxO3a/Bim axis in chronic lymphocytic leukemia cells. Haematologica. 2013 Nov;98(11):1739-47. doi: 10.3324/haematol.2013.088849. Epub 2013 Jul 12. PubMed PMID: 23850807; PubMed Central PMCID: PMC3815175.

7: Zang C, Eucker J, Liu H, Coordes A, Lenarz M, Possinger K, Scholz CW. Inhibition of pan-class I phosphatidyl-inositol-3-kinase by NVP-BKM120 effectively blocks proliferation and induces cell death in diffuse large B-cell lymphoma. Leuk Lymphoma. 2014 Feb;55(2):425-34. doi: 10.3109/10428194.2013.806800. Epub 2013 Jul 25. PubMed PMID: 23721513.

8: Ren H, Zhao L, Li Y, Yue P, Deng X, Owonikoko TK, Chen M, Khuri FR, Sun SY. The PI3 kinase inhibitor NVP-BKM120 induces GSK3/FBXW7-dependent Mcl-1 degradation, contributing to induction of apoptosis and enhancement of TRAIL-induced apoptosis. Cancer Lett. 2013 Sep 28;338(2):229-38. doi: 10.1016/j.canlet.2013.03.032. Epub 2013 Apr 2. PubMed PMID: 23562472; PubMed Central PMCID: PMC3750077.

9: Kirstein MM, Boukouris AE, Pothiraju D, Buitrago-Molina LE, Marhenke S, Schütt J, Orlik J, Kühnel F, Hegermann J, Manns MP, Vogel A. Activity of the mTOR inhibitor RAD001, the dual mTOR and PI3-kinase inhibitor BEZ235 and the PI3-kinase inhibitor BKM120 in hepatocellular carcinoma. Liver Int. 2013 May;33(5):780-93. doi: 10.1111/liv.12126. Epub 2013 Mar 15. PubMed PMID: 23489999.

10: Amrein L, Shawi M, Grenier J, Aloyz R, Panasci L. The phosphatidylinositol-3 kinase I inhibitor BKM120 induces cell death in B-chronic lymphocytic leukemia cells in vitro. Int J Cancer. 2013 Jul;133(1):247-52. doi: 10.1002/ijc.27989. Epub 2013 Jan 15. PubMed PMID: 23238639; PubMed Central PMCID: PMC3847963.

Additional Information

944396-07-0 (free base)
1312445-63-8 (HCl).

NVP-BKM120 is a selective pan class 1 PI3 Kinase inhibitor.  It was found that NVP-BKM120 inhibited the PI3 signaling pathways, leading to different forms of cell death based on P53 statuses. Further studies are warranted to determine if NVP-BKM120 has potential as a glioma treatment. (source: http://www.ncbi.nlm.nih.gov/pubmed/22065080 ).