KA001-1
4-(Pyrrolidin-1-ylmethyl)aniline hydrochloride
Price: 1g = $240.00
2.5g = $480.00

KA002-1
4-((Diethylamino)methyl)aniline hydrochloride
1g = $240.00
2.5g = $480.00

KA003-1
4-(2-(Pyrrolidin-1-yl)ethyl)aniline hydrochloride
1g = $240.00
2.5g = $480.00

KA005
4-Piperidin-1-ylmethyl-phenylamine
1g = $300.00
2.5g = $600.00

KA006
4-Morpholin-4-ylmethyl-phenylamine
1g = $300.00
2.5g = $600.00

KA007
4-(4-Methyl-piperazin-1-ylmethyl)-phenylamine
1g = $300.00
2.5 = $600.00

KA015
4-(2-Piperidin-1-yl-ethyl)-phenylamine
1g = $220.00
2.5g = $440.00

KA016
4-(2-Morpholin-4-yl-ethyl)-phenylamine
1g = $300.00
2.5g = $600.00

KA017
4-[2-(4-Methyl-piperazin-1-yl)-ethyl]-phenylamine
1g = $300.00
2.5g = $600.00

KA025
73-[(4-amino-phenylamino)-pyrrolidine-1-carboxylic acid tert-butyl ester
1g = $300.00
2.5g = $600.00

KA026
3-[(4-amino-phenylamino)-pyrrolidine-1-carboxylic acid tert-butyl ester
1g = $300.00
2.5g = $600.00

KA027
4-(4-amino-phenylamino)- piperidine-1-carboxylic acid tert-butyl ester
1g = $245.00
2.5g = $490.00

KA028
4-[(4-amino-phenylamino)-methyl]-piperidine-1-carboxylic acid
1g = $300.00 2.5g = $600.00

KA029
3-(4-amino-phenylamino)- piperidine-1-carboxylic acid tert-butyl ester
1g = $260.00
2.5g = $520.00

KA030
3-[(4-amino-phenylamino)-methyl]- piperidine-1-carboxylic acid tert-butyl ester
1g = $265.00
2.5g = $530.00

KA031
2-[(4-amino-phenylamino)-methyl]- piperidine-1-carboxylic acid tert-butyl ester
1g = $300.00
2.5g = $600.00

KA032-1
2-(4-amino-phenylamino)- piperidine-1-carboxylic acid benzyl ester hydrochloride
1g = $300.00
2.5g = $600.00

1. Noronha, Glenn; Cao, Jianguo; Chow, Chun P.; Mak, Chi Ching; Palanki, Moorthy S. S.; Dneprovskaia, Elena; McPherson, Andrew; Pathak, Ved Prakash; Renick, Joel; Zeng, Binqi. Preparation of pyrrolopyrimidine compounds and their use as janus kinase modulators. WO 2009049028 To view article, click here.

In a recently published Targegen patent, aminoanilines are used in the exocyclic position of a pyrrolopyrimidine core. Products derived from KA005 and KA006 showed improved cellular activity, <500 nM, over other heterocycles at the same position.

2. Tsou, Hwei-Ru; Otteng, Mercy; Tran, Tritin; Floyd, M. Brawner, Jr.; Reich, Marvin; Birnberg, Gary; Kutterer, Kristina; Ayral-Kaloustian, Semiramis; Ravi, Malini; Nilakantan, Ramaswamy; Grillo, Mary; McGinnis, John P.; Rabindran, Sridhar K.4-(Phenylaminomethylene)isoquinoline-1,3(2H,4H)-diones as Potent and Selective Inhibitors of the Cyclin-Dependent Kinase 4 (CDK4). Journal of Medicinal Chemistry (2008), 51(12), 3507-3525 To view article, click here.

In this article, 4,6-substituted isoquinolinediones as selective inhibitors of CDK4 are described by scientists from Wyeth. Potency varied by more than 20 fold depending on the nature of the aniline derived 4 substituent. The same position also had a significant effect on the solubility and selectivity of the final products. In the proposed binding model, the piperidine nitrogen provided by the KA005 starting material interacts with an aspartate on the enzyme.

3. Li, Rongshi; Xue, Liquan; Zhu, Tong; Jiang, Qin; Cui, Xiaoli; Yan, Zheng; McGee, Danny; Wang, Jian; Gantla, Vidyasagar Reddy; Pickens, Jason C.; McGrath, Doug; Chucholowski, Alexander; Morris, Stephan W.; Webb, Thomas R.Design and Synthesis of 5-Aryl-pyridone-carboxamides as Inhibitors of Anaplastic Lymphoma Kinase. Journal of Medicinal Chemistry  (2006), 49(3), 1006-1015 To view article, click here.

A solid phase synthesis of ALK inhibitors used 4-substituted anilines as amide coupling partners in the last variable step. Changes in both activity and selectivity were observed between the piperazinylaniline and the derivatives separated by 0-3 methylenes. The preferred substitution was the n=1 derivative, from starting material KA007, which gave both good potency and better selectivity versus kinases like IGF1R.

4. Khire, Uday; Liu, Xiao-Gao; Nagarathnam, Dhanapalan; Wood, Jill; Wang, Lei; Liu, Donglei; Zhao, Jin; Guernon, Leatte; Zhang, Lei. . Quinolone carboxylic acid derivatives for treatment of hyperproliferative conditions, their preparation and pharmaceutical compositions. WO 2005097752 To view article, click here.

Quinolones are well known antibiotics, but in a recent Bayer Pharmaceuticals patent the antitumor activity of this drug class is highlighted. Substitution of the quinolone nitrogen with aromatic groups derived from KA starting materials generates a series of compounds that prevent carcinoma cell growth. Although the target is not disclosed, compound IC50’s are often less than 500 nM when the aniline contains a basic center like that found in KA001-1.