In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 370 pM
The EGFR is a 170-kDa protein that contains an extracellular ligand binding domain, a single transmembrane domain, and an intracellular tyrosine kinase domain. EGF-R is hyperactivated in numerous tumors including those derived from the lung, brain, bladder, prostate, head, and neck. It has been shown previously that 4-anilino quinazolines compete with the ability of ATP binding the EGFR, inhibit EGF-stimulated autophosphorylation of tyrosine residues in EGFR, and block EGF-mediated growth. CL-387785 is an irreversible inhibiter of EGFR.
In vitro: CL-387785 covalently bound to EGFR. It also specifically inhibited kinase activity of the protein, blocked EGF-stimulated autophosphorylation of the receptor in cells, inhibited cell proliferation primarily in a cytostatic manner in cell lines that overexpress EGF-R or c-erbB-2 .
In vivo: The effects of CL-387785 on tumor growth were assessed in human tumor xenografts implanted s.c. in the flanks of nude mice. CL-387785 inhibited the growth of tumors derived from A431 cells when the drug was administered i.p. or p.o.. Inhibitory effects were observed within 7 days after the onset of therapy. No efficacy was observed with CL-387785 in tumors derived from cell lines that did not overexpress EGF-R, including the human breast carcinoma MDA-MB-435 .
Clinical trial: Up to now, CL-387785 is still in the preclinical development stage.
 Discafani CM, Carroll ML, Floyd MB Jr, Hollander IJ, Husain Z, Johnson BD, Kitchen D, May MK, Malo MS, Minnick AA Jr, Nilakantan R, Shen R, Wang YF, Wissner A, Greenberger LM. Irreversible inhibition of epidermal growth factor receptor tyrosine kinase with in vivo activity by N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-2-butynamide (CL-387,785). Biochem Pharmacol. 1999 Apr 15;57(8):917-25.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||insoluble in EtOH; insoluble in H2O; ≥16.85 mg/mL in DMSO|
|Shipping Condition||Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.|
|General tips||For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.|