CI-1040 Inhibitor CAS No. 212631-79-3

Cat. No.	Name	Size	Price
KI0387	CI-1040	5 mg	$112
	CI-1040	10 mg	$192
	CI-1040	25 mg	$432
	CI-1040	100 mg	$1072
	CI-1040	200 mg	$1232

Chemical Characteristic

Product Name	CI-1040
Synonyms	PD184352
CAS No.	212631-79-3
Molecular Weight	478.67
Formula	C₁₇H₁₄ClF₂IN₂O₂
Chemical Name	2-(2-chloro-4-iodophenylamino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide
Smiles	C(=O)(c1c(c(c(cc1)F)F)Nc1c(cc(cc1)I)Cl)NOCC1CC1
Chemical Structure

Biological activities

CI-1040 is a small-molecule with highly selective adenosine triphosphate (ATP) non-competitive inhibition activity against MEK1/2. CI-1040 directly inhibits MEK1 with a 50% inhibitory concentration (IC50) of 17 nM, without affecting the activity of mitogen-activated protein kinase (MAPK). However, CI-1040, at concentrations as high as 10 µM, does not substantially inhibit MKK3, protein kinase C, cyclin dependent kinase 2A, phosphorylase kinase, EGF receptor kinase, PDGF receptor kinase and c-src. CI-1040 (as low as 100 nM) totally inhibits MAPK phorylation induced by platelet-derived growth factor (PDGF) in colon 26 carcinoma cells. 1 µM CI-1040 produces a reduction of steady-state levels of phosphorylated MAPK of more than 75% in colon 26 carcinoma cells. Besides, identical results are obtained with many tumor lines of human origin, including BX-PC3 pancreatic, A431 cervical, HT-29 colon, ZR-75-1 breast and SKOV-3 ovarian carcinomas. 10 µM CI-1040 does not inhibit the phosphorylation of Jun kinase, p38 kinase or AKT. CI-1040 produces a dose-dependent block in the G1 phase of the cell cycle in colon 26 cells. The percentage of cells in G1 is 45% for the DMSO-treated control cells and increases to 59%, 73% and 84% after treatment of cells for 24 hours with CI-1040 at final concentrations of 0.1, 1 and 10 µM, respectively. CI-1040 inhibits anchorage-independent growth in a dose-dependent manner, with an IC50 of 0.15 µM in colon 26 cells. In vivo colon 26 carcinoma tumor model, either intraperitoneally or orally with CI-1040 at a dose of 150 mg/kg completely suppresses MAPK phosphorylation for at least 6 hours. Then, MAPK phosphorylation returns at 12 hours after dosing, and attains control levels by 24 hours. In another colon 26 carcinoma xenograft model, tumor growth is inhibited 53??9% with a wide dose range of CI-1040 (48-200mg/kg per dose). In human colon carcinoma HT-29 xenografts, CI-1040 elicits similar growth inhibition (59??9%) of HT-29 tumors at all of the dosages (48-200mg/kg per dose).^[1]

Protocols

CI-1040 is prepared in a vehicle of 10% Cremophore EL, 10% ethanol and 80% water. ^[1]

References

[1] Sebolt-Leopold JS, et al. Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo. Nat Med. 1999, 5(7):810-816.

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