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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/AKN-028/1/205942
产品编号:205942
市  场 价:¥0.00
场      地:美国(厂家直采)
产品分类: 蛋白类>多肽>多肽合成>
联系QQ:1570468124
电话号码:4000-520-616
邮      箱: info@ebiomall.com
美  元  价:待定
品      牌: MedKoo
公      司:MedKoo Biosciences, Inc
公司分类:
MedKoo/AKN-028/1/205942
商品介绍

AKN-028

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

MedKoo CAT#:205942

CAS#:1175017-90-9

Description:AKN-028, the FLT3/KIT kinase inhibitor, is an orally bioavailable protein tyrosine kinase inhibitor for FMS-related tyrosine kinase 3 (FLT3; STK1) and stem cell factor receptor (SCFR; KIT), with potential antineoplastic activity. FLT3/KIT kinase inhibitor AKN-028 binds to and inhibits both the wild-type and mutated forms of FLT3 and SCFR. This may result in an inhibition of tumor cell proliferation in cancer cell types that overexpress these receptor tyrosine kinases. Check for active clinical trials or closed clinical trials using this agent.

Price and Availability

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

AKN-028,is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.

Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205942Name: AKN-028CAS#: 1175017-90-9Chemical Formula: C17H14N6Exact Mass: 302.12799Molecular Weight: 302.33Elemental Analysis: C, 67.54; H, 4.67; N, 27.80

Synonym:AKN-028; AKN 028; AKN028

IUPAC/Chemical Name:N2-(1H-indol-5-yl)-6-(pyridin-4-yl)pyrazine-2,3-diamine

InChi Key:JLRIJKVMMZEKDF-UHFFFAOYSA-N

InChi Code:InChI=1S/C17H14N6/c18-16-17(22-13-1-2-14-12(9-13)5-8-20-14)23-15(10-21-16)11-3-6-19-7-4-11/h1-10,20H,(H2,18,21)(H,22,23)

SMILES Code:NC1=NC=C(C2=CC=NC=C2)N=C1NC3=CC4=C(NC=C4)C=C3

Technical Data

Appearance:
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:
>5 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

AKN-028, a novel tyrosine kinase inhibitor (TKI), is a potent FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor (IC(50)=6 nM), causing dose-dependent inhibition of FLT3 autophosphorylation. Inhibition of KIT autophosphorylation was shown in a human megakaryoblastic leukemia cell line overexpressing KIT. In a panel of 17 cell lines, AKN-028 showed cytotoxic activity in all five AML cell lines included. AKN-028 triggered apoptosis in MV4-11 by activation of caspase 3. In primary AML samples (n=15), AKN-028 induced a clear dose-dependent cytotoxic response (mean IC(50) 1 μM). However, no correlation between antileukemic activity and FLT3 mutation status, or to the quantitative expression of FLT3, was observed. Combination studies showed synergistic activity when cytarabine or daunorubicin was added simultaneously or 24 h before AKN-028. In mice, AKN-028 demonstrated high oral bioavailability and antileukemic effect in primary AML and MV4-11 cells, with no major toxicity observed in the experiment. (source: Blood Cancer J. 2012 Aug 3;2:e81. doi: 10.1038/bcj.2012.28.)   

References

1: Eriksson A, Hermanson M, Wickström M, Lindhagen E,Ekholm C, Jenmalm Jensen A, Löthgren A, Lehmann F, Larsson R, Parrow V,Höglund M. The novel tyrosine kinase  inhibitor AKN-028 hassignificant antileukemic activity in cell lines and primary cultures ofacute myeloid leukemia. Blood Cancer J. 2012 Aug 3;2:e81. doi:10.1038/bcj.2012.28. PubMed PMID: 22864397; PubMed Central PMCID:PMC3432483.

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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