| Size | Price | Stock | Qty |
|---|---|---|---|
| 2mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
CL-387785 (CL387785; WAY-EKI 785; EKI 785; EKI785) is a novel, potent, covalent / irreversible, and selective EGFR inhibitor with potential anticancer activity. CL-387785 functions by covalently binding to EGFR and preventing EGF-stimulated autophosphorylation of the receptor in cells (IC50 = approximately 5 nM). This inhibits cell proliferation (IC50 = 31-125 nM), mainly in a cytostatic manner in cell lines that overexpress EGF-R or c-erbB-2. Furthermore, it significantly blocked the growth of a tumor in nude mice that overexpresses EGF-R.
| Targets |
EGFR (IC50 = 370 pM)
|
|---|---|
| ln Vitro |
CL-387785 inhibits cell proliferation (IC50, 31 nM) mainly by cytostatic means in cell lines that overexpress EGF-R or c-erbB-2. It also blocks EGF-stimulated autoposphorylation of the receptor in cells (IC50, 5 nM).[1]
|
| ln Vivo |
CL-387785 (80 mg/kg/day, p.o.) significantly inhibits tumor growth in nude mice overexpressing EGF-R. In rodent models of autosomal recessive polycystic kidney disease (ARPKD), administering CL-387785 (90 mg/kg, intraperitoneally) to Balb/c-bpk/bpk (BPK) mice leads to a notable decrease in collecting tubule cystic lesions, enhanced renal function, a reduction in biliary epithelial abnormalities, and an extension of life span.[2] The growth of the HCA-7-induced xenograft tumor is inhibited by doses of CL-387785 as low as 25 mg/kg, and tumor growth is completely prevented at 100 mg/kg. The HCT-116-induced xenograft tumor can be effectively inhibited in growth by a dose of 50 mg/kg CL-387785.[5]
|
| Enzyme Assay |
After being prepared in 100% DMSO, 500 μM CL-387785 stock solutions are diluted with 30 mM HEPES, pH 7.4, to achieve the desired concentration. After dilution to 1:120 in 100 mM HEPES, pH 7.4, 10 microliters of CL-387785 at different concentrations are incubated for 10 minutes on ice with 3 μL of recombinant enzyme. Afterwards, 5 μL of peptide (400 μM final concentration of RR-SRC made up of Arg-Arg-Leu-Ile-Glu-Asp-Ala-Glu-Tyr-Ala-Ala-Arg-Gly), 10 μL of 4× reaction buffer with pH 7.4, 50 mM HEPES, 80 μM ATP, 40 mM MnCl2, and 200 μM sodium orthovanadate were added. 12.0 μL H2O and 0.30 μL [33P]ATP (>2500 Ci/mmol) are added. The entire volume is spotted onto precut P81 filter sheets following a 90-minute room temperature incubation period. A liquid scintillation counter is used to measure radioactivity after the filter discs are twice cleaned with 0.5% phosphoric acid. EGF-R kinase's specific activity is roughly 0.50 pmol/mg/min in these circumstances.
|
| Cell Assay |
The CellTiter 96@AQueous One solution proliferation kit is used to conduct MTS assays. For 48 hours, different inhibitor concentrations are incubated with 10,000 cells per well in 96-well flat-bottomed plates. Using XL⨁t4, the IC50 is calculated from dose–response curves.
|
| Animal Protocol |
Human CRC cell line xenografts (nude mice)
100 mg/kg i.p. |
| References |
| Molecular Formula |
C18H13BRN4O
|
|
|---|---|---|
| Molecular Weight |
717.18
|
|
| Exact Mass |
380.03
|
|
| Elemental Analysis |
C, 56.71; H, 3.44; Br, 20.96; N, 14.70; O, 4.20
|
|
| CAS # |
194423-06-8
|
|
| Related CAS # |
|
|
| Appearance |
Solid powder
|
|
| SMILES |
CC#CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=CC=C3)Br
|
|
| InChi Key |
BTYYWOYVBXILOJ-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C18H13BrN4O/c1-2-4-17(24)22-14-7-8-16-15(10-14)18(21-11-20-16)23-13-6-3-5-12(19)9-13/h3,5-11H,1H3,(H,22,24)(H,20,21,23)
|
|
| Chemical Name |
N-[4-(3-bromoanilino)quinazolin-6-yl]but-2-ynamide
|
|
| Synonyms |
EKI785; CL 387785; EK-I785; EK I785; WAY-EKI 785; CL387785; CL-387785; WAY-EKI785; WAY-EKI-785
|
|
| HS Tariff Code |
2934.99.9001
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3944 mL | 6.9718 mL | 13.9435 mL | |
| 5 mM | 0.2789 mL | 1.3944 mL | 2.7887 mL | |
| 10 mM | 0.1394 mL | 0.6972 mL | 1.3944 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 |
|---|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA