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主营:抗癌化学试剂和激酶抑制剂
℡ 4000-520-616
℡ 4000-520-616
MedKoo/Buparlisib (BKM120)featured/100mg/204690
产品编号:204690
市  场 价:¥3000.00
场      地:美国(厂家直采)
产品分类: 蛋白类>多肽>多肽合成>
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美  元  价:$150.00
品      牌: MedKoo
公      司:MedKoo Biosciences, Inc
公司分类:
MedKoo/Buparlisib (BKM120)featured/100mg/204690
商品介绍

Buparlisib (BKM120)
featured

WARNING: This product is for research use only, not for human or veterinary use.

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.

Price and Availability

SizePriceShipping out timeQuantity
100mgUSD 150Same day
200mgUSD 250Same day
500mgUSD 450Same day
1gUSD 850Same day
2gUSD 1450Same day
5gUSD 2450Same day
10gUSD 3950Same day
20gUSD 6950Same day
50gUSD 99502 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-01-23.Prices are subject to change without notice.

Buparlisib, purity > 98%, is in stock. The same day shipping out after order is received.

Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 204690Name: Buparlisib (BKM120)CAS#: 944396-07-0 (free base)Chemical Formula: C18H21F3N6O2Exact Mass: 410.16781Molecular Weight: 410.39Elemental Analysis:C, 52.68; H, 5.16; F, 13.89; N, 20.48; O, 7.80

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 Key:CWHUFRVAEUJCEF-UHFFFAOYSA-N

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)

SMILES Code:NC1=NC=C(C2=NC(N3CCOCC3)=NC(N4CCOCC4)=C2)C(C(F)(F)F)=C1

Technical Data

Appearance:
white solid powder

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

Certificate of Analysis:
View CoA: current batch, Lot#SSC60123

QC Data:
View QC data: current batch, Lot#SSC60123

Safety Data Sheet (SDS):
View Safety Data Sheet (SDS)

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

Additional Information

Related: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 ).    

References

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 advancedsolid 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, SatoM, Kakizume T, Robson M, Quadt C, Doi T. Phase I dose-escalation studyof buparlisib (BKM120), an oral pan-class I PI3K inhibitor, in Japanesepatients 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 PI3Kinhibitor NVP-BKM120 on acquired resistance to gefitinib of human lungadenocarcinoma H1975 cells. J Huazhong Univ Sci Technolog Med Sci. 2013Dec;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, LocatelliF, McCubrey JA, Barata JT, Martelli AM. Activity of the pan-class Iphosphoinositide 3-kinase inhibitor NVP-BKM120 in T-cell acutelymphoblastic 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 hereditaryhemorrhagic telangiectasia after treatment with the phosphoinositide3-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-BKM120overcomes resistance signals derived from microenvironment by regulatingthe 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-BKM120effectively blocks proliferation and induces cell death in diffuse largeB-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-dependentMcl-1 degradation, contributing to induction of apoptosis andenhancement of TRAIL-induced apoptosis. Cancer Lett. 2013 Sep28;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, MarhenkeS, Schütt J, Orlik J, Kühnel F, Hegermann J, Manns MP, Vogel A. Activityof the mTOR inhibitor RAD001, the dual mTOR and PI3-kinase inhibitorBEZ235 and the PI3-kinase inhibitor BKM120 in hepatocellular carcinoma.Liver Int. 2013 May;33(5):780-93. doi: 10.1111/liv.12126. Epub 2013 Mar15. PubMed PMID: 23489999.

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

品牌介绍
MedKoo,由化学家和药学家陈清奇博士。北卡罗莱纳州的研究三角区(Research Triangle Park, 简称 RTP ),是一家以研发、生产和销售小分子抗癌化合物为主的医药科技公司,该公司的业务范围主要是为全球所有从事抗癌药物研究和开发的制药公司,高校,研究院所,政府相关机构提供与抗癌药物分子相关的产品、试剂和技术服务。
中文名MedKoo中    文美帝药库医药科技公司创立于2008年总部位于美国东海岸
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