[CAS NO. 183321-74-6] Erlotinib (OSI-774)

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [183321-74-6]

Catalog

SLK-S7786

Brand

Selleck

CAS

183321-74-6

DESCRIPTION [183321-74-6]

Overview

MDL	MFCD08063588
Molecular Weight	393.44
Molecular Formula	C22H23N3O4
SMILES	N(C=1C2=C(C=C(OCCOC)C(OCCOC)=C2)N=CN1)C3=CC(C#C)=CC=C3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.5417 mL	12.7084 mL	25.4168 mL
5 mM	0.5083 mL	2.5417 mL	5.0834 mL
10 mM	0.2542 mL	1.2708 mL	2.5417 mL
50 mM	0.0508 mL	0.2542 mL	0.5083 mL

Description

Erlotinib (OSI-774, CP358774, NSC 718781, Tarceva) is an inhibitor with of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces .

Targets

EGFR ^[1]
(Cell-free assay)

2 nM

In vitro

Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 20nM), DiFi human colon cancer cells and MDA MB-468 human breast cancer cells. Erlotinib HCl (1 μM) induces apoptosis in DiFi human colon cancer cells. Erlotinib inhibits growth of a panel of NSCLC cell lines including A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 with IC50 ranging from 29 nM to >20 μM. Erlotinib HCl(2 μM) significantly inhibits growth of AsPC-1 and BxPC-3 pancreatic cells. The effects of Erlotinib HCl in combination with gemcitabine are considered additive in KRAS-mutated pancreatic cancer cells. Ten micromolar of Erlotinib HCl inhibits EGFR phospho-rylation at the Y845 (Src-dependent phosphorylation) and Y1068 (auto-phosphorylation) sites. Combination with Erlotinib HCl could down-modulate rapamycin-stimulated Akt activity and produces a synergistic effect on cell growth inhibition.

In vivo

At doses of 100 mg/kg, Erlotinib HCl completely prevents EGF-induced autophosphorylation of EGFR in human HN5 tumors growing as xenografts in athymic mice and of the hepatic EGFR of the treated mice. Erlotinib HCl (100 mg/Kg) inhibits H460a and A549 tumor models with 71 and 93% inhibition rate.

References

[1] Moyer JD, et al. Cancer Res. 1997, 57(21), 4838-4848.
[2] Li T, et al. Clin Cancer Res, 2007, 13(11), 3413-3422.
[3] Ali S, et al. Mol Cancer Ther, 2008, 7(6), 1708-1719.
[4] Buck E, et al. Mol Cancer Ther. 2006, 5(11), 2676-2784.
[5] Higgins B, et al. Anticancer Drugs. 2004, (5), 503-512.
[6] Furugaki K,et al. Oncol Lett. 2010, 1(2), 231-235.
[7] Bago-Horvath Z, et al. 2012, DOI: 10.1159/000337257

Synonyms

4-Quinazolinamine, N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-

N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine

OSI 744

Erlotinib

NSC 718781

R 1415

4-[(3-Ethynylphenyl)amino]-6,7-bis(2-methoxyethoxy)quinazoline