Custom Premix Selecting "Custom Premix" option means that all of the beads you have chosen will be premixed in manufacturing before the kit is sent to you.
A cell-permeable pyrimidylpyrrole compound that acts as an active site-targeting, highly potent and selective ERK1/2 inhibitor (KI <2 nM against Erk2; [ATP] = 65 µM), while inhibiting GSK-3, Aurora A, Cdk2 only at much higher concentrations (KI = 395, 540, and 852 nM, respectively) and exhibiting much reduced or little potency toward a panel of more than 130 other kinases (KI ≥1.4 µM; IC50 ≥1 µM). Shown to effectively inhibit human colon carcinoma HT-29 proliferation (IC50 = 48 nM) and restore EGFR inhibitor WZ4002 antiproliferation activity in WZR10 cultures (84% and no inhibition, respectively, by 100 nM WZ4002 with or without 1 µM Erk Inhibitor VIII co-treatment). Orally available in both mice and rats in vivo.
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas
Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
产品目录编号
GTIN
328011-10MGCN
04055977195620
Documentation
ERK Inhibitor VIII, VX-11e - CAS 896720-20-0 - Calbiochem 分析证书
标题
批号
328011
参考
参考信息概述
Ercan, D., et al. 2012. Cancer Discovery2, 934. Aronov, A.M., et al. 2009. J. Med. Chem.52, 6362.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
A cell-permeable pyrimidylpyrrole compound that acts as an active site-targeting, highly potent and selective ERK1/2 inhibitor (KI <2 nM against Erk2; [ATP] = 65 µM), while inhibiting GSK-3, Aurora A, Cdk2 only at much higher concentrations (KI = 395, 540, and 852 nM, respectively) and exhibiting much reduced or little potency toward a panel of more than 130 other kinases (KI ≥1.4 µM; IC50 ≥1 µM). Shown to effectively inhibit human colon carcinoma HT-29 proliferation (IC50 = 48 nM) and be orally available in both mice (F = 67%; t1/2 = 4.4 h; Plasma conc. = 488 and 122 ng/mL, respectively, 4 h and 8 h post single 33 mg/kg oral dosage) and rats (F = 65%; t1/2 = 3 h; Plasma conc. = 329 and 267 ng/mL, respectively, 4 h and 8 h post single 10 mg/kg oral dosage) in vivo. Also reported to restore EGFR inhibitor WZ4002 antiproliferation activity in WZR10 cultures (84% and no inhibition, respectively, by 100 nM WZ4002 with or without 1 µM Erk Inhibitor VIII co-treatment).
Form
Yellowish-white powder
Intert gas (Yes/No)
Packaged under inert gas
CAS number
896720-20-0
Chemical formula
C₂₄H₂₀Cl₂FN₅O₂
Structure formula
Purity
≥98% by Chiral HPLC
Solubility
DMSO (50 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity
Standard Handling
References
Ercan, D., et al. 2012. Cancer Discovery2, 934. Aronov, A.M., et al. 2009. J. Med. Chem.52, 6362.
