(3,5-Bis(trifluoromethyl)phenyl)(ethyl)sulphane
Supplier:
Adipogen
Description:
AS703026 is a novel, selective, non-competitive, orally bioavailable MEK1/2 inhibitor with experimental IC(50) values of 5-11nM. In use on multiple myeloma cells (MM), AS703026 inhibited growth and survival of MM cells and cytokine-induced osteoclast differentiation more potently (~10X) than AZD6244. Inhibition of proliferation induced by AS703026 was mediated by G0-G1 cell cycle arrest and was accompanied by reduction of MAF oncogene expression. AS703026 further induced apoptosis via caspase 3 and Poly ADP ribose polymerase (PARP) cleavage in MM cells, both in the presence or absence of bone marrow stromal cells (BMSCs). Importantly, AS703026 sensitized MM cells to a broad spectrum of conventional (dexamethasone, melphalan), novel or emerging (lenalidomide, perifosine, bortezomib, rapamycin) anti-MM therapies. Significant tumour growth reduction in AS703026- vs. vehicle-treated mice bearing H929 MM xenograft tumours correlated with downregulated pERK1/2, induced PARP cleavage, and decreased microvessels in vivo. Moreover, AS703026 (<lt/>200nM) was cytotoxic against the majority of tumour cells tested from patients with relapsed and refractory MM (84%), regardless of mutational status of RAS and BRAF genes. Importantly, BMSC-induced viability of MM patient cells was similarly blocked within the same dose range.
Catalog Number:
(97064-490)
Supplier:
Adipogen
Description:
AV-412 is a potent dual inhibitor of EGFR and ErbB2 tyrosine kinases, including the mutant EGFR(L858R,T790M), which is clinically resistant to the EGFR-specific kinase inhibitors erlotinib and gefitinib. In enzyme assays assay the compound inhibited the EGFR variants and ErbB2 in the nanomolar range with over 100-fold selectivity compared with other kinases, apart from ABL and FLT1, which were both moderately sensitive to the compound. In cells, AV-412 inhibited autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively. It also inhibited epidermal growth factor (EGF)-dependent cell proliferation with an IC(50) of 100nM. Moreover, AV-412 abrogated EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR. In animal studies using cancer xenograft models, AV-412 (30mg/kg) demonstrated complete inhibition of tumor growth of the A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively.
Catalog Number:
(BDH83627.400)
Supplier:
VWR International
Description:
BDH* Chloroform (Ethanol Stabilized), Chemical Formula: CHCl3, Melting Point: -63.6, Boiling Point: 61.1, Flash Point: N/A, Formula Weight: 119.38, CAS Number: 67-66-3, Grade: HPLC/Spectro, HiPerSolv CHROMANORM, Class: F, Size: 4L
Catalog Number:
(BDH7393-2)
Catalog Number:
(BDH83624.400)
Supplier:
VWR International
Description:
BDH* Ethyl Ether (Ethanol Stabilized), Chemical Formula: C4H10O, Melting Point: -116.3, Boiling Point: 34.5, Flash Point: -45 deg C, Formula Weight: 74.12, CAS Number: 60-29-7, Grade: HPLC/Spectro, HiPerSolv CHROMANORM, Class: F, Size: 4L
Supplier:
MilliporeSigma
Description:
Emplura* Ethanol absolute, Cas number: 64-17-5, Chemical Formula:C2H5OH, Solvent for lab application, 1l.
Catalog Number:
(77401-198)
Supplier:
APOLLO SCIENTIFIC
Description:
Ethanol-[D₆] (>99.0% D)
Supplier:
AMBEED, INC
Description:
(R)-1-(2-Chlorophenyl)ethanol 97%
Supplier:
AMBEED, INC
Description:
α-(4-Isobutylphenyl)ethanol 97%
Supplier:
AMBEED, INC
Description:
1-(2-Naphthyl)ethanol 98%
Supplier:
THERMO FISHER SCIENTIFIC CHEMICALS
Description:
Ethanol absolute ≥99.5% ACS (200 Proof)
Supplier:
Adipogen
Description:
The kinases called p38 MAP kinases (MAPKs) are intracellular, soluble serine-threonine kinases which belong to a large family of proteins that include the extracellular regulated kinases (ERKs) and c-Jun N-terminal kinases (JNKs). So far four p38 isoforms have been identified, namely p38alpha, p38beta, p38gamma and p38delta, a.k.a. p38-alpha (MAPK14), -beta (MAPK11), -gamma (MAPK12 / ERK6), and -delta (MAPK13 / SAPK4). The ubiquitously expressed s p38alpha has been the most extensively studied and is believed to be the most physiologically relevant in the regulation of the inflammatory response. The role of the three other isoforms is not currently well understood, however their primary sites of expression are known. Similar to p38alpha, p38beta is also ubiquitously expressed, while p38gamma is expressed predominately in skeletal muscle and p38delta is expressed primarily in the lung, kidney, testis, small intestine and pancreas. The small molecule inhibitor VX-702 is a potent p38 kinase family inhibitor that has been studied for its effects on inflammation and the inflammatory response. VX-702 dose-dependently inhibited the production o IL-6, IL-1beta and TNFalpha (IC(50) = 59, 122 and 99ng/ml, respectively), and in anti-platelet aggregation assays, pre-incubation of platelets with VX-702 (1µM)completely or partially inhibited platelet agonist induced p38 activation (IC(50) = 4 to 20nM). More recently VX-702 has been studied as a potential treatment for rheumatoid arthritis (RA). VX-702 appears to be most effective against MAPK14, followed by MAPK11 and the remaining members of the family, however exact in vitro IC(50) values have not been published. However a large amount of data is available for in vitro growth inhibition assays where VX-702 exhibits poptent activity, having low IC(50) values beginning at ~16nM and ending at < 400µM for the numerous cell lines tested.
Supplier:
VWR International
Description:
Safety-vented wash bottles provide compliance with the Globally Harmonized System of Classification and Labeling of Chemicals (GHS) and OSHA’s HazCom 2012 requirements - as pertains to 'Workplace Labels'.
Catalog Number:
(77401-196)
Supplier:
APOLLO SCIENTIFIC
Description:
Ethanol-[D₁] (>99,5% D)
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