Cellagen Technology: New Products - PI3k/Akt/mTOR

RAD001 (Everolimus) | mTOR inhibitor

Sat, 15 Jun 2013 20:41:31 +0000

RAD001 (Everolimus) is an orally-bioavailable, semi-synthetic mTOR inhibitor with immunosuppressive activity. It has an IC50 against FKBP12 (FK506-binding protein 12) of 1.8-2.6 nM. Moreover, in an IL-6-dependent hybridoma clone, growth factor-stimulated cell proliferation was measured at an IC..

Price: $89.00

GDC-0349 | mTOR inhibitor

Sat, 15 Jun 2013 20:40:09 +0000

GDC-0349 is an ATP-competitive, potent and selective inhibitor of mTOR with an Ki value of 3.8 nM. It has ~800-fold selectivity over PI3Ka and in PC3 cells exhibits an EC50 of 270 nM. Additionally GDC-0349 showed less than 25% inhibition in a panel of 266 kinases, including all isoforms of..

Price: $119.00

BX-912 | PDK1 inhibitor

Sat, 15 Jun 2013 20:39:43 +0000

BX-912 is an aminopyrimidine-based, ATP-competitive inhibitor of PDK1 at an IC50 of 12 nM. In a panel of relevant serine-threonine and receptor-tyrosine kinases, BX-912 showed at least 20-fold selectivity with the exception of 9-fold selectivity (110 nM) for PKA. In a panel of cell lines, BX-91..

Price: $169.00

WYE125132 | mTOR inhibitor

Thu, 16 May 2013 03:12:03 +0000

WYE125132 is an orally-available, ATP-competitive, pyrazolopyrimidine-based, specific inhibitor of mTORC1 and mTORC2 with an mTOR potency of 0.19 nM and >5000-fold selectivity against the PI3K isoform family, hSMG1, and ATR enzymes. WYE125132 selectively inhibits phosphorylation of p-Akt (S4..

Price: $159.00

GDC-0980 (RG7422) | PI3K/mTOR inhibitor

Thu, 16 May 2013 03:11:17 +0000

GDC0980, a orally-available, thienopyrimidine-based, ATP-competitive dual inhibitor of PI3K class I isoforms (IC50 of 5, 27, 7, and 14 nM for PI3Ka, b, d, and g) and mTOR (Ki of 17 nM). [1&91; GDC0980 potently inhibits signal transduction (Thr308, Ser473) downstream of both PI3K and mTOR and showe..

Price: $149.00

PS48 | PDK1 inhibitor

Wed, 13 Mar 2013 11:35:56 +0000

PS48 is an allosteric small molecule activator of phosphoinositide-dependent protein kinase 1 (PDK1). It binds to the HM/PIF binding pocket instead of the ATP-binding site. PS48 has been used to enhance reprogramming of neonatal human epidermal keratinocytes (NHEKs).

Techn..

Price: $79.00

BIBF1120 (Vargatef, Nintedanib) | VEGFR/PDGFR/FGFR inhibitor

Wed, 13 Mar 2013 07:56:45 +0000

BIBF1120 (Vargatef, Nintedanib) is an oxindole-based, orally-available triple kinase inhibitor targeting the angiogenesis factors VEGF, PDGF, and FGF. It inhibits VEGFR, PDGFR, and FGFR at potency ranges of 13-34, 59-65, and 37-108 nM. [1&91; Kinase panel studies show that it also inhibits Flt-3, ..
Price: $129.00

XL147 | PI3K inhibitor

Wed, 13 Mar 2013 07:51:43 +0000

XL147 is an orally-available, reversible and competitive ATP inhibitor of the PI3K class of kinases with potencies of 39 nM, 36 nM, and 23 nM, for isoforms PI3Ka, PI3Kd, PI3Kg, respectively. [1&91; It is highly selective versus mTOR (>15000 nM) and DNA-PK (4750 nM). and a broad panel of >130..
Price: $129.00

PP242 | mTOR inhibitor

Wed, 13 Mar 2013 07:50:59 +0000

PP242 is an ATP-competitive, pyrazolopyrimidine-based inhibitor of mTOR at an IC50 of 8 nM. It is highly selective against the PI3K family of kinases, with all but one isoform (p110g IC50 = 102 nM) registering with IC50s > 1 uM. In a broad kinase panel, PP242 showed modest activity only in P..
Price: $89.00

PKI-587 | PI3K/mTOR inhibitor

Wed, 13 Mar 2013 07:50:54 +0000

PKI587 (PF-05212384) is a ATP-competitive, triazine-based, orally-bioavailable dual PI3K/mTOR inhibitor with potencies of 0.4 nM and 1.0 nM, respectively. [1&91; PKI587 is highly selective over a panel of 236 human protein kinases (IC50 > 10 uM)It inhibits growth over over 50 human tumor cell l..
Price: $169.00