Erlotinib HCl (OSI-744) - 2mM in DMSO , Epidermal growth factor receptor erbB1 inhibitor, CAS No.183319-69-9, Epidermal growth factor receptor erbB1 inhibitor

CAS: 183319-69-9 Cat. No.: E409025 Molecular Weight: 429.9 EC Number: 620-491-0
AVAILABLE TO ORDER
GRADE & PURITY 2mM in DMSO
Synonyms
CP358774, NSC 718781
Storage
Store at -80°C
Shipped In
Dry ice packs + Cold packs
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Size
Status
Price
Qty
1ml
E409025-1ml
2
$56.90
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Why this grade

2mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.

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Storage & shipping

Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.

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Quality documents

SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.

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Literature proof

Cited in 4 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.

Overview

Information


In vitro

Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 20nM), DiFi humancolon cancer cells andMDA MB-468 human breast cancer cells. Erlotinib HCl (1 μM) induces apoptosis in DiFi humancolon 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.
Cell Data

cell lines:

Concentrations:30 nM-20 μM

Incubation Time:72 hours

Powder Purity:≥99%

Specifications

Synonyms
CP358774, NSC 718781
Specifications & Purity
2mM in DMSO
Biochemical and Physiological Mechanisms
Erlotinib HCl (OSI-744, CP358774, NSC 718781) is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
Storage
Store at -80°C
Shipped In
Dry ice packs + Cold packs
This product requires cold chain shipping. Ground and other economy services are not available.
Action Type
INHIBITOR
Mechanism of action
Epidermal growth factor receptor erbB1 inhibitor
Names and Identifiers
Isomeric SMILES COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC.Cl
Alternate CAS 183319-69-9
NSC Number 718781
MeSH Entry Terms 11C erlotinib;11C-erlotinib;358,774, CP;358774, CP;CP 358,774;CP 358774;CP-358,774;CP-358774;CP358,774;CP358774;erlotinib;erlotinib HCl;erlotinib hydrochloride;HCl, Erlotinib;Hydrochloride, Erlotinib;N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-
Molecular Weight 429.9
Reaxy-Rn 8813963
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8813963&ln=

Documentation

📋 Safety Data Sheet (SDS)

Comprehensive hazard, handling, storage, and regulatory compliance document.

Download SDS →

✅ Certificate of Analysis (COA)

Lot-specific quality data. Enter your lot number to retrieve the exact COA.

Look up COA →

📊 Datasheet

Quick-reference summary of product specifications and applications.

View datasheet →

🔬 Specification Sheet

Full quality attributes and acceptance criteria for this grade.

View spec sheet →

Advanced Data

Certificates(CoA,COO,BSE/TSE and Analysis Chart)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Chemical and Physical Properties
SolubilitySolubility (25°C) In vitro DMSO: 75 mg/mL (293.8 mM); Water: 75 mg/mL (293.8 mM); Ethanol: 75 mg/mL warmed with 50ºC Water: bath (293.8 mM);
Melt Point(°C)228 °C
Documents & Articles
Citations of This Product
References
1. Yun Zheng, Qiong Zhao, Jing Lin, Xiaoyang Dai, Chenyu Zhu, Yujie Wang, Hongye Fu.  (2022)  Xijiao Dihuang decoction relieves the erlotinib-induced dermatitis.  EXPERIMENTAL CELL RESEARCH,      [PMID:36435221] [10.1016/j.yexcr.2022.113437]
2. Yuping Liu, Xiangliang Jiang, Yue Gu, Yan Chen.  (2019)  Preventive effect of Diallyl Trisulfide on cutaneous toxicities induced by EGFR inhibitor.  INTERNATIONAL IMMUNOPHARMACOLOGY,      [PMID:30682720] [10.1016/j.intimp.2019.01.023]
3. Yueying Zhang, Dan Gao, Shangfu Li, Weili Wei, Jinshun Lin, Yuyang Jiang.  (2019)  1,5-Diaminonaphthalene functionalized carbon nanodots as a novel matrix for the analysis of small molecules by matrix-assisted laser desorption/ionization mass spectrometry.  Analytical Methods,  11  (8): (1131-1136).  [PMID:] [10.1039/C8AY02665C]
4. Xiaolan Zhou, Xiaofeng Zhu, Weixu Wang, Jing Wang, Haimei Wen, Yuqi Zhao, Jiayu Zhang, Qiushi Xu, Zhaozhao Zhao, Ting Ni.  (2025)  Comprehensive Cellular Senescence Evaluation to Aid Targeted Therapies.  Research,      [PMID:39822281] [10.34133/research.0576]
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