3-(4-Methylphenyl)-1H-pyrazole
Supplier:
TCI America
Description:
[for Biochemical Research]
CAS Number: 22198-72-7 MDL Number: MFCD00042012 Molecular Formula: C11H13N3O Molecular Weight: 239.70 Purity/Analysis Method: >98.0% (HPLC,T) Form: Crystal
Catalog Number:
(76481-006)
Supplier:
AAT BIOQUEST INC
Description:
Monochloromobimane (mBCl) is essentially nonfluorescent until reacted with a thiol group.
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Supplier:
Adipogen
Description:
LY2784544 is a potent JAK2 inhibitor with IC(50) of 3nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2.
Supplier:
Adipogen
Description:
AMG-458 is a potent inhibitor of c-Met with an IC(50) of 60nM and displays selectivity against VEGFR2.
Supplier:
Adipogen
Description:
AG13958 is a VEGF inhibitor that was in clinical development for treatment of age-related macular degeneration (AMD). The drug displays low water solubility and so far in trials delivery has been difficult needing direct injection to be truly effective and it varied by the species used because of species specific differences in eye circulation and vascularization. As a VEGF inhibitor AG13958 was targeted to FLT/TYK receptor inhibition.
Supplier:
Adipogen
Description:
Inhibitor of pan-Trk activity (IC(50) = 8 and 12nM for TrkA and TrkB). Shown to target Trk (tropomyosin receptor kinase) ATP binding cleft and an immediately adjacent hydrophobic pocket. Preferentially arrests the proliferation of Ba/F3 cells fused with Tel-TrkA, Tel-TrkB and Tel-TrkC (IC(50) = 11, 9 and 7nM, respectively) and in Ba/F3 and RIE cells expressing both TrkA and NGF (IC(50) = 42 and 17nM, respectively) over Mo7e-c-Kit and Rat-A10-PDGFR (IC(50) = 1 and 0.5µM) and Ba/F3-Tel-KDR and wt-Ba/F3 cells (IC(50) = 3.0 and 5.6µM). Displays ~100-fold greater selectivity among a panel of 59 closely related kinases and in 33 cellular kinase assays. Weakly active against relevant cytochrome P450 isozymes and hERG channel, and exhibit adequate microsomal stability, pharmacokinetic profile and efficacy in mice and rats. Suppresses tumor growth in a mouse RIE-TrkAmNGF xenograft model (50mg/kg, p.o.).
Supplier:
Adipogen
Description:
XL765 is active against class I PI3K (IC(50) = 39, 113, 9 and 43nM for p110alpha, beta, gamma and delta, respectively). XL765 also inhibits DNA-PK (IC(50) = 150nM) and mTOR (IC(50) = 157nM)
Supplier:
TCI America
Description:
1-Nitropyrazole, Purity: >97.0%(GC), CAS number: 7119-95-1, Molecular Formula: C3H3N3O2, Molecular Weight: 113.08, Form: Crystal - Powder, White - Slightly pale yellow, Size: 5G
Catalog Number:
(EM1.03133.0025)
Catalog Number:
(102541-576)
Supplier:
Matrix Scientific
Description:
MF=C20H18N4O4 MW=378.39 CAS=152120-55-3 MDL=MFCD02092983 5G
Catalog Number:
(101801-196)
Supplier:
Matrix Scientific
Description:
Matrix Scientific Part Number: 011725-500MG , MDL Number: MFCD06801330
Supplier:
Adipogen
Description:
Antineoplastic, anti-inflammatory and immunomodulating agent. Orally bioavailable potent ATP mimetic that inhibits both JAK1 and JAK2 with IC50 values of 2.7 and 4.5nM, respectively and is less selective for JAK3 (IC50=322nM). Affects DC differentiation and function, leading to impaired T cell activation. Used in the treatment of myeloproliferative neoplasms and psoriasis. Anticancer agent. Shown to induce apoptosis and autophagy. Potent and selective inhibitor of HIV-1 replication and virus reactivation in vitro.
Catalog Number:
(101793-658)
Supplier:
Matrix Scientific
Description:
Matrix Scientific Part Number: 007919-500MG , MDL Number: MFCD00996156
Supplier:
Adipogen
Description:
Antagonizing the Chk1-mediated cell cycle checkpoints has emerged as an attractive target for anticancer therapy. If Chk1 activity is blocked, DNA-damaged or spindle-disrupted cells would exit cell cycle arrest before full repair and subsequently undergo mitotic catastrophe or cell death. Chk1 inhibitors consequently increase the therapeutic index of DNA-damaging or antimitotic agents as well. PF-0477736 is a selective, potent ATP-competitive Chk1 inhibitor, derived from PF-0394691, inhibits Chk1 (Ki, 0.49nM) and Chk2 (Ki, 47nM) in vitro. In tests, PF-0477736 was identified as a potent, selective ATP-competitive small-molecule inhibitor that inhibits Chk1 with a Ki of 0.49nM. PF-0477736 abrogates cell cycle arrest induced by DNA damage and enhances cytotoxicity of clinically important chemotherapeutic agents, including gemcitabine and carboplatin. In xenografts, PF-0477736 enhanced the antitumor activity of gemcitabine in a dose-dependent manner. PF-0477736 combinations were well tolerated with no exacerbation of side effects commonly associated with cytotoxic agents.
Supplier:
Adipogen
Description:
Tozasertib, or VX-680, is a potent and selective inhibitor of Aurora kinases, particularly Aurora A and B. In vitro, VX-680 blocks cell cycle progression and induces apoptosis in a wide range of human tumor types at low IC(50) values (i.e. 3.38nM for human BE-13 cells, and 14.34nM for NTERA cells). Moreover, VX680, also has very potent Ki values, with inhibition constants (Ki) of 0.6, 18, and 46nM for Aurora A, B, and C, respectively. VX-680 is also effective in vivo, being used in a Caki-1 xenograft model, VX-680 demonstrated a 75.7% (P < 0.001) decrease in Caki-1 xeno-graft tumor volume with no apparent alternation in animal body weight, peripheral blood counts, or other biological parameters.
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.
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