4-(1,3-Benzothiazol-2-yl)phenylamine
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.
Supplier:
ALADDIN SCIENTIFIC
Description:
2-(2-Aminothiazol-4-yl)acetic acid ≥98% (by HPLC)
Supplier:
Adipogen
Description:
The lymphocyte-specific kinase (Lck) is a cytoplasmic tyrosine kinase of the Src family expressed in T cells and natural killer (NK) cells. Genetic evidence in both mice and humans demonstrates that Lck kinase activity is critical for signaling mediated by the T cell receptor (TCR), which leads to normal T cell development and activation. Selective inhibition of Lck is expected to offer a new therapy for the treatment of T-cell-mediated autoimmune and inflammatory disease. AMG-47 is one of two optimized chemical compounds that has been shown to be extremely effective in vivo and in vitro in inhibiting Lck as well as a number of other receptor tyrosine kinases. In an anti-CD3/ IL-2 mouse model system AMG-47 has been shown to be effective in inhibiting the Lck mediated anti-inflammatory activity (ED50 11 mg/kg; 630nM) in vivo. In multiple other in vitro assays, AMG-47 exhibits subnanomolar inhibition against Lck, and low (<lt/>10nM) inhibition against other hard to inhibit kinases such as KDR and SRC and MAPK alpha (p38alpha). Moreover at slightly higher doses but well under 10µM, AMG-47 effectively inhibits the JNK family of kinases including TYK2 at ~ 1.2µM.
Supplier:
AMBEED, INC
Description:
3-(1-Piperazinyl)-1,2-benzisothiazole, Purity: 95%, CAS Number: 87691-87-0, Appearance: Form: Crystal - Powder / Colour: Very pale yellow - Yellow, Storage: Inert atmosphere, 2-8C, Size: 10G
Catalog Number:
(102531-194)
Supplier:
Matrix Scientific
Description:
MF=C6H9NOS MW=143.21 CAS=137-00-8 MDL=MFCD00005339 100G
Supplier:
AMBEED, INC
Description:
2-(4-Methyl-5-thiazolyl)ethyl decanoate 98%
Supplier:
Strem Chemicals Inc
Description:
Pincer Ligands and Complexes, Pybox
Catalog Number:
(77878-810)
Supplier:
AMBEED, INC
Description:
N-(2-Oxoethyl)phthalimide 98%
Supplier:
Strem Chemicals Inc
Description:
Pincer Ligands and Complexes, Pybox
Supplier:
Adipogen
Description:
AT7519 is a potent inhibitor of several CDK family members. AT7519 showed potent antiproliferative activity (40-940nM) in a panel of human tumor cell lines, and the mechanism of action was shown here to be consistent with the inhibition of CDK1 and CDK2 in solid tumor cell lines. AT7519 caused cell cycle arrest followed by apoptosis in human tumor cells and inhibited tumor growth in human tumor xenograft models. Tumor regression was observed following twice daily dosing of AT7519 in the HCT116 and HT29 colon cancer xenograft models. Also it has been shown that the biological effects are linked to inhibition of CDKs in vivo and that AT7519 induces tumor cell apoptosis in these xenograft models. Moreover, AT7519 has an attractive biological profile and is well tolerated and effective making it a more plausible candidate for clinical development than previously available CDK inhibitors. In in vitro kinase assays AT7519 showed nanomolar levels of activity from <lt/>10 to 2400 for cyclins; only one other non-cyclin related kinase was inhibited at levels below 10µM (GSK3beta, 89nM), all others tested had IC(50)'s of greater than 10,000nM.
Supplier:
Matrix Scientific
Description:
MF=C23H19N3O2 MW=369.43 CAS=128249-70-7 MDL=MFCD01863585 10G
Supplier:
Matrix Scientific
Description:
MF=C23H19N3O2 MW=369.43 CAS=174500-20-0 MDL=MFCD01863586 1G
Supplier:
Thermo Scientific Chemicals
Description:
250mg CAS: 53218-26-1, MDL: MFCD04115372
Supplier:
AMBEED, INC
Description:
2-(2-Aminothiazol-4-yl)acetic acid, Purity: 99%, CAS Number: 29676-71-9, Appearance: Solid, Storage: Keep in dark place, Inert atmosphere, 2-8C, Size: 25G
Supplier:
AMBEED, INC
Description:
4-Methyl-5-thiazoleethanol, Purity: 95%, CAS Number: 137-00-8, Appearance: Solid or semi-solid or lump or liquid, Storage: Sealed in dry, Room Temperature, Size: 10g
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