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MedKoo/Capivasertibfeatured/10mg/205669

  • 产品编号: 205669
  • 美  元  价: $150.00
  • 市  场  价: ¥3000.00
  • 品       牌:
  • 产       地: 美国(厂家直采)
  • 公       司: MedKoo Biosciences, Inc
  • 产品分类:
  • 公司分类: Angiogenesis
MedKoo/Capivasertibfeatured/10mg/205669
  • MedKoo/Capivasertibfeatured/10mg/205669
商品介绍

Capivasertib
featured

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

MedKoo CAT#:205669

CAS#:1143532-39-1

Description:AZD5363, also known as Capivasertib, is an orally available inhibitor of the serine/threonine protein kinase AKT (protein kinase B) with potential antineoplastic activity. AKT inhibitor AZD5363 binds to and inhibits all AKT isoforms. Inhibition of AKT prevents the phosphorylation of AKT substrates that mediate cellular processes, such as cell division, apoptosis, and glucose and fatty acid metabolism. A wide range of solid and hematological malignancies show dysregulated PI3K/AKT/mTOR signaling due to mutations in multiple signaling components.

Price and Availability

SizePriceShipping out timeQuantity
10mgUSD 150Same day
25mgUSD 250Same day
50mgUSD 450Same day
100mgUSD 750Same day
200mgUSD 1250Same day
500mgUSD 1950Same day
1gUSD 26502 Weeks
2gUSD 38502 Weeks
5gUSD 69502 Weeks
Inquire bulk and customized quantity

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

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

Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205669Name: CapivasertibCAS#: 1143532-39-1Chemical Formula: C21H25ClN6O2Exact Mass: 428.17275Molecular Weight: 428.9152Elemental Analysis:C, 58.81; H, 5.87; Cl, 8.27; N, 19.59; O, 7.46

Synonym:AZD5363; AZD-5363; AZD 5363; Capivasertib

IUPAC/Chemical Name:(S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide

InChi Key:JDUBGYFRJFOXQC-KRWDZBQOSA-N

InChi Code:InChI=1S/C21H25ClN6O2/c22-15-3-1-14(2-4-15)17(6-12-29)27-20(30)21(23)7-10-28(11-8-21)19-16-5-9-24-18(16)25-13-26-19/h1-5,9,13,17,29H,6-8,10-12,23H2,(H,27,30)(H,24,25,26)/t17-/m0/s1

SMILES Code:O=C(C1(N)CCN(C2=C3C(NC=C3)=NC=N2)CC1)N[C@H](C4=CC=C(Cl)C=C4)CCO

Technical Data

Appearance:
white solid powder

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

Certificate of Analysis:
View CoA: current batch, Lot#C9R04B23

QC Data:
View QC data: current batch, Lot#C9R04B23

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

AZD5363 is  a novel pyrrolopyrimidine derived compound which inhibited all AKT isoforms with a potency of <10 nM, and inhibited phosphorylation of AKT substrates in cells with a potency of ~0.3 to 0.8 µM. AZD5363 monotherapy inhibited the proliferation of 41/182 solid and hematologic tumor cell lines with a potency of <3 µM. Cell lines derived from breast cancers showed the highest frequency of sensitivity. There was a significant relationship between the presence of PIK3CA and/or PTEN mutations and sensitivity to AZD5363, and between RAS mutations and resistance. Oral dosing of AZD5363 to nude mice caused dose- and time-dependent reduction of PRAS40, GSK3β and S6 phosphorylation in BT474c xenografts (PRAS40 phosphorylation EC50 ~0.1 µM total plasma exposure), reversible increases in blood glucose concentrations and dose-dependent decreases in fluorodeoxyglucose (FDG) uptake in U87-MG xenografts. Chronic oral dosing of AZD5363 caused dose-dependent inhibition of the growth of xenografts derived from various tumor types, including HER2+ breast cancer models that are resistant to trastuzumab. AZD5363 also significantly enhanced the antitumor activity of docetaxel, lapatinib and trastuzumab in breast cancer xenografts. It is concluded that AZD5363 is a potent inhibitor of AKT with pharmacodynamic activity in vivo, has potential to treat a range of solid and hematologic tumors as monotherapy or a combinatorial agent, and has potential for personalized medicine based on the genetic status of PIK3CA, PTEN and RAS. AZD5363 is currently in phase I clinical trials. (source: Mol Cancer Ther molcanther.0824.2011)   

References

1: Toren P, Kim S, Cordonnier T, Crafter C, DaviesBR, Fazli L, Gleave ME, Zoubeidi A. Combination AZD5363 withEnzalutamide Significantly Delays Enzalutamide-resistant Prostate Cancerin Preclinical Models. Eur Urol. 2014 Aug 20. pii:S0302-2838(14)00748-9. doi: 10.1016/j.eururo.2014.08.006. [Epub ahead ofprint] PubMed PMID: 25151012.

2: Li J, Davies BR, Han S, Zhou M, Bai Y, Zhang J, Xu Y, Tang L, Wang H,Liu YJ, Yin X, Ji Q, Yu DH. The AKT inhibitor AZD5363 is selectivelyactive in PI3KCA mutant gastric cancer, and sensitizes a patient-derivedgastric cancer xenograft model with PTEN loss to Taxotere. J Transl Med.2013 Oct 2;11:241. doi: 10.1186/1479-5876-11-241. PubMed PMID: 24088382;PubMed Central PMCID: PMC3850695.

3: Addie M, Ballard P, Buttar D, Crafter C, Currie G, Davies BR,Debreczeni J, Dry H, Dudley P, Greenwood R, Johnson PD, Kettle JG, LaneC, Lamont G, Leach A, Luke RW, Morris J, Ogilvie D, Page K, Pass M,Pearson S, Ruston L. Discovery of4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potentinhibitor of Akt kinases. J Med Chem. 2013 Mar 14;56(5):2059-73. doi:10.1021/jm301762v. Epub 2013 Feb 26. PubMed PMID: 23394218.

4: Maynard J, Ricketts SA, Gendrin C, Dudley P, Davies BR.2-Deoxy-2-[18F]fluoro-D-glucose positron emission tomographydemonstrates target inhibition with the potential to predict anti-tumouractivity following treatment with the AKT inhibitor AZD5363. Mol ImagingBiol. 2013 Aug;15(4):476-85. doi: 10.1007/s11307-013-0613-3. PubMedPMID: 23344784.

5: Lamoureux F, Thomas C, Crafter C, Kumano M, Zhang F, Davies BR,Gleave ME, Zoubeidi A. Blocked autophagy using lysosomotropic agentssensitizes resistant prostate tumor cells to the novel Akt inhibitorAZD5363. Clin Cancer Res. 2013 Feb 15;19(4):833-44. doi:10.1158/1078-0432.CCR-12-3114. Epub 2012 Dec 20. PubMed PMID: 23258740.

6: Davies BR, Greenwood H, Dudley P, Crafter C, Yu DH, Zhang J, Li J,Gao B, Ji Q, Maynard J, Ricketts SA, Cross D, Cosulich S, Chresta CC,Page K, Yates J, Lane C, Watson R, Luke R, Ogilvie D, Pass M.Preclinical pharmacology of AZD5363, an inhibitor of AKT:pharmacodynamics, antitumor activity, and correlation of monotherapyactivity with genetic background. Mol Cancer Ther. 2012Apr;11(4):873-87. doi: 10.1158/1535-7163.MCT-11-0824-T. Epub 2012 Jan31. PubMed PMID: 22294718.

品牌介绍


MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务。

MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务和分子有竞争力的价格。MedKoo是您可靠的合作伙伴采购药物发现和药物分子。




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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。
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