Cellagen Technology LLC
 
작성일 : 16-10-12
[Cellagen Technology LLC] Disease Area, Oncology I
A-674563 l PPKB/Akt inhibitor / Abiraterone l P450 CYP17 inhibitor / ABT-263 (Navitoclax) l Bcl-2 family inhibitor / ABT-737 | Apoptosis inhibitor

 

Disease Area, Oncology I

 

 

Product Name: A-674563 l PKB/Akt inhibitor (#C2167)

 

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A-674563 is a potent and selective PKB/Akt inhibitor with an IC50 of 14 nM. It binds to ATP-binding site of Akt

and reduces the phosphorylation of Akt's downstream targets (GSK3α/β, FOXO3, TSC2, mTOR and S6, etc.).

A-674563 also inhibits activity of PKA and CDK2 with IC50 of 16 and 46 nM, respectively. A-674563 inhibits

proliferation of tumor cells with IC50 of 0.4 µM1.

In STS cells, A-674563 induces Akt pathway blockade that decreases downstream target phosphorylation,

and induces G2 cell cycle arrest and apoptosis. In vivo, A-674563 reduces STS xenograft growth2. When

given in combination, A-674563 enhanced the efficacy of paclitaxel in a PC-3 xenograft model1.

 

Details

Chemical Formula:

 

C22H22N4O

CAS No.:

 

552325-73-2

Molecular weight:

 

358.44

Purity:

> 98%

Appearance:

 

White solid

Chemical name:

 

(2S)-1-(5-(3-methyl-1H-indazol-5-yl)pyridin-3-yloxy)-3-phenylpropan-2-amine

Solubility:

 

Up to 100 mM in DMSO

Storage:

   

For longer shelf life, store solid powder at 4oC desiccated, or DMSO solution

at -20oC

 

References

1. Furuta et al., T-705 (favipiravir) and related compounds: Novel broad-spectrum inhibitors of RNA viral

   infections. Antiviral Res. 2009, 82, 95-102. Pubmed ID: 19428599   

2. Kiso et al., T-705 (favipiravir) activity against lethal H5N1 influenza A viruses. Proc. Natl. Acad. Sci.

   2010, 107(2), 882-887. Pubmed ID: 20080770

 

 

Product Name: Abiraterone l P450 CYP17 inhibitor (#C2247)

 

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Abiraterone is a potent steroidal inhibitor against cytochrome P450 17alpha-hydroxylase-17,20-lyase (CYP17)

with an IC50 at 4 nM. It was approved by the FDA in April 2011 to treat castration-resistant prostate cancer. A

phase I/II clinical trial evaluating abiraterone acetate in advanced breast cancer patients are also underway.

In preclinical studies, abiraterone has demonstrated the ability to selectively inhibit the target enzyme,

resulting in inhibition of testosterone production in both the adrenals and the testes.

 

Details

Chemical Formula:

 

C24H31NO

CAS No.:

 

154229-19-3

Molecular weight:

 

349.51

Purity:

> 98%

Appearance:

 

White solid

Chemical name:

 

 

(3S,8R,9S,10R,13S,14S)-10,13-dimethyl-17-(pyridin-3-yl)-

2,3,4,7,8,9,10,11,12,13,14,15-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol

Solubility:

 

Up to 50 mM in DMSO

Storage:

   

For longer shelf life, store solid powder at 4oC desiccated, or DMSO solution

at -20oC

 

References

1. Attard G et al. Selective inhibition of CYP17 with abiraterone acetate is highly active in the treatment of

   castration-resistant prostate cancer. J Clin Oncol. 2009;27(23):3742-8.

2. Attard G et al. Phase I clinical trial of a selective inhibitor of CYP17, abiraterone acetate, confirms that

   castration-resistant prostate cancer commonly remains hormone driven. J Clin Oncol. 2008;26(28):4563-71.

 

 

Product Name: ABT-263 (Navitoclax) | Bcl-2 family inhibitor (#C2263)

 

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ABT-263 is an orally-available Bcl-2 family inhibitor with Ki values of < 1 nM for Bcl-2, Bcl-xL, and Bcl-w.

ABT-263 disrupts key Bcl interactions with proteins such as Bim, inducing apoptosis. Despite being a Bad-

like Bh3 mimetic, ABT-263 has been shown to possess cytotoxic activity and induce apoptosis based

primarily on its Bcl-2 family inhibitory activity.

ABT-263 as a standalone agent has modest activity in lymphoma and myeloma xenografts, but is extremely

effective in enhancing the efficacy of clinically relevant therapies such as rituxumab and bortezomib. (1)

In a panel of small cell lung cancer (SCLC) xenografts, including H146, H889, and H1963 models, ABT-263

displays excellent antitumor effects, leading to tumor regression. (2)

 

Details

Chemical Formula:

 

C47H55ClF3N5O6S3

CAS No.:

 

923654-51-6

Molecular weight:

 

947.61

Purity:

> 98%

Appearance:

 

White

Chemical name:

 

   

 

(R)-4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)

piperazin-1-yl)-N-((4-((4-morpholino-1-(phenylthio)butan-2-yl)amino)-3-

((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide

Solubility:

 

Up to 100 mM in DMSO

Synonyms:

 

ABT-263, Navitoclax, ABT263, ABT 263

Storage:

 

 

For longer shelf life, store solid powder at 4oC desiccated, or DMSO solution

at -20oC

 

References

1. Tse et al., ABT-263: A Potent and Orally Bioavailable Bcl-2 Family Inhibitor. Cancer Res. 2008, 68,

   3421-3428. Pubmed ID: 18451170   

2. Shoemaker et al., Activity of the Bcl-2 Family Inhibitor ABT-263 in a Panel of Small Cell Lung Cancer

   Xenograft Models. Clin. Cancer Res. 2008, 14, 3268-3277. Pubmed ID: 18519752

 

 

Product Name: ABT-737 | Apoptosis inhibitor (#C2281)

 

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ABT-737 is a selective and potent small molecule inhibitor of protein Bcl-2, Bcl-XL, and Bcl-w. Like a BAD

BH3 peptide, ABT-737 binds to and antagonizes anti-apototic Bcl-2 family proteins instead of directly

activating the apoptotic process. ABT-737 binds with high affinity (ki < 1nm) to Bcl-XL, Bcl-2 and Bcl-w, but

not to Bcl-B, Mcl-1 and Al protein.

ABT-737 displays a wide range of single-agent activity against cells from lymphoma, leukemia, solid tumor

SCLC, and primary cells derived from patient. In animal models, ABT-737 causes tumor regression and

improves survival1-2. ABT-737 has shown synergistic anti-tumor activity when used together with vorinostat

or bemicitabine3,4.

 

Details

Chemical Formula:

 

C42H45ClN6O5S2

CAS No.:

 

852808-04-9

Molecular weight:

 

813.43

Purity:

> 98%

Appearance:

 

Off White solid

Chemical name:

  

   

 

4-[4-[(4'-Chloro[1,1'-biphenyl]-2-yl)methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-

(dimethylamino)-1-[(phenylthio)methyl]propyl]amino]-3-nitrophenyl]sulfonyl]

benzamide

Solubility:

 

Up to 50 mM in DMSO

Storage:

   

For longer shelf life, store solid powder at 4oC desiccated, or DMSO solution

at -20oC

 

References

1. Oltersdorf, T. et al. An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Nature.

   2005 Jun 2;435(7042):677-81.

2. Van Deelft , MF. et al. The BH3 mimetic ABT-737 targets selective Bcl-2 proteins and efficiently induces

   apoptosis via Bak/Bax if Mcl-1 is neutralized. Cancer Cell. 2006 Nov;10(5):389-99.

3. Zhang, C. et al. Synergistic anti-tumor activity of gemcitabine and ABT-737 in vitro and in vivo through

   disrupting the interaction of USP9X and Mcl-1. Mol Cancer Ther. 2011 Jul;10(7):1264-75.

4. Wiegmans AP, et al. Deciphering the molecular events necessary for synergistic tumor cell apoptosis

   mediated by the histone deacetylase inhibitor vorinostat and the BH3 mimetic ABT-737. Cancer Res. 2011

 

 


Ordering informations

    

Catalog No.

Product Name

Size

C2167

A-674563 l PPKB/Akt inhibitor

2 mg, 10 mg & 50 mg

C2247

Abiraterone l P450 CYP17 inhibitor

2 mg, 10 mg & 50 mg

C2263

ABT-263 (Navitoclax) l Bcl-2 family inhibitor

5 mg, 25 mg & 100 mg

C2281

ABT-737 | Apoptosis inhibitor

5 mg, 25 mg & 100 mg

 



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