Erlotinib hydrochloride|cas 183319-69-9|DC Chemicals

Cas No.:	183319-69-9
Chemical Name:	Erlotinib hydrochloride
Synonyms:	N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine hydrochloride;ERLOTINIB;ERLOTINIB HCL SALT;TARCEVA;ERLOTINIB HCL SALT :TARCEVA;Erlotinib, Hydrochloride Salt;N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-;quinazolinamine, Hydrochloride Salt, OSI 774, Tarceva;N-(3-Ethynylphenyl)-6,7-bis-(2-methoxyethoxy)-quinazolin-4-amine;[6,7-Bis-(2-methoxy-ethoxy)-quinazolin-4yl]-(3-ethynyl-phenyl)-amine;Tarceva Hydrochloride See E625000;Erlotinib HCl;Erlotinib hydrochloride;Erlotinib HCl (OSI-744);[6,7-Bis-(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)-amine;Erlotinib Hydrochlorid;Erlotinib Hydrochloride (Tarceva);Erlotinib, Hydrochloride Salt (Tarceva®);N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-quinazolin-4-amine hydrochloride;Tarceva (Erlotinib Hydrochloride);(±)-Cloprostenol; 6,7-Bis(2-methoxyethoxy)-4-(3-ethynylanilino)quinazoline hydrochloride;CP-358774;Erlotinib (Hydrochloride);Erlotinib,OS-774;Erlotinib-d6 HCl;Erlotonid HCl;NSC 718781;OSI 774;OSI-774;774 hydrochloride;CP-358;N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride;OSI-744 hydrochloride;N-(3-Ethynylphenyl)[6,7-bis(2-methoxyethoxy)quinazolin-4-yl]amine hydrochloride;RG-1415;CP 358774;RO-0508231;CP-358774-01;DA87705X9K;4-Quinazolinamine, N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-, hydrochloride (1:1);6,7-bis(2-methoxyethoxy)-4-(3-ethynylanilino)quinazoline hcl;(CP358774;N-(3-ethynylphenyl)-6,7
SMILES:	Cl[H].O(C([H])([H])C([H])([H])OC([H])([H])[H])C1C([H])=C2C(=NC([H])=NC2=C([H])C=1OC([H])([H])C([H])([H])OC([H])([H])[H])N([H])C1=C([H])C([H])=C([H])C(C#C[H])=C1[H]
Formula:	C₂₂H₂₄ClN₃O₄
M.Wt:	429.8967
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Erlotinib hydrochloride inhibits purified EGFR kinase with an IC50 of 2 nM.
In Vivo:	There is a 1.49-fold statistically significant difference between AUC0-inf after p.o. administration of Erlotinib (5 mg/kg) comparing Bcrp1/Mdr1a/1b-/- and WT mice (7,419±1,720 versus 4,957±1,735 ng*h/mL respectively, P=0.01)[3]. The administration of Erlotinib (10 mg/kg/day, or 20 mg/kg/day) to Bleomycin (BLM)-treated rats shows no exacerbation of lung injuries in indices such as macroscopic findings, lung weights, histopathological scores (lung lesion density and lung fibrosis score), and pulmonary hydroxyproline (HyP) level. The result suggests that Erlotinib does not have any exacerbating effects on lung injuries induced by BLM in rats[4].
In Vitro:	Erlotinib (CP-358,774) Hydrochloride is also a potent inhibitor of the recombinant intracellular (kinase) domain of the EGFR, with an IC50 of 1 nM. The proliferation of DiFi cells is strongly inhibited by Erlotinib with an IC50 of 100 nM for an 8-day proliferation assay[1]. The combination of B-DIM and Erlotinib (2 μM) results in a significant inhibition of colony formation in BxPC-3 cells when compared with either agent alone. The combination of B-DIM and Erlotinib (2 μM) results in a significant induction of apoptosis only in BxPC-3 cells when compare with the apoptotic effect of either agent alone[2].

Cat. No.	Product name	Field of application
DC10479	RX518(CK-101:EGFR-IN-3)	RX518(CK-101) is an orally available third-generation and selective inhibitor of certain epidermal growth factor receptor (EGFR) activating mutations.
DC1091	PF-299804 (Dacomitinib,PF-00299804)	PF299804 is a potent, irreversible pan-ErbB inhibitor against ErbB1, ErbB2 and ErbB4 with IC50 of 6 nM, 45.7 nM and 73.7 nM, respectively.
DC7225	Pelitinib (EKB-569; WAY-EKB 569)	Pelitinib (EKB-569; WAY-EKB 569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM.
DC11900	Lazertinib	Lazertinib (YH25448, GNS-1480) is a highly potent, mutant-selective, irreversible, brain-penetrant and orally active EGFR tyrosine-kinase inhibitors for both the T790M mutation and activating EGFR mutations
DC2103	Gefitinib (ZD1839)	Gefitinib (Iressa, ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively.
DC3139	Erlotinib hydrochloride	Erlotinib HCl is an HER1/EGFR inhibitor with IC50 of 2 nM.
DC2101	Erlotinib free base	Erlotinib (OSI-744; NSC 718781; R1415) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
DC7106	Rociletinib (CO-1686)	CO-1686 is a novel, irreversible and orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M(IC50=21 nM).
DC3138	Canertinib dihydrochloride	Canertinib dihydrochloride is the hydrochloride salt of an orally bio-available quinazoline with potential antineoplastic and radiosensitizing activities.
DC8462	AZD-9291 mesylate (Osimertinib，Mereletinib)	AZD-9291 is a potent and selective mutated forms EGFR inhibitor(Exon 19 deletion EGFR IC50=12.92 nM, L858R/T790M EGFR IC50= 11.44 nM, wild type EGFR IC50= 493.8 nM).