EGFR-IN-48

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EGFR-IN-48

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

EGFR-IN-48 是一种有效的且具有口服活性的EGFR抑制剂，对 EGFR^d19/TM/CS, EGFR^LR/TM/CS, EGFR^WT的IC₅₀值分别为 0.193 nM, 0.251 nM, 10.4 nM。EGFR-IN-48 抑制 BaF3^{EGFR del19/T790M/C797S}和 PC-9^{EGFR del19/T790M/C797S}细胞的增殖，IC₅₀值分别为 1.526 nM 和 66.7 nM。

生物活性

EGFR-IN-48 is a potent and orally activeEGFRinhibitor withIC₅₀s of 0.193 nM, 0.251 nM, 10.4 nM forEGFR^d19/TM/CS,EGFR^LR/TM/CS,EGFR^WT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3^{EGFRdel19/T790M/C797S}and PC-9^{EGFRdel19/T790M/C797S}cells with IC₅₀s of 1.526, 66.7 nM, respectively^[1].

IC₅₀& Target

EGFR^d19/TM/CS

0.193 nM (IC₅₀)

EGFR^LR/TM/CS

0.251 nM (IC₅₀)

EGFR^WT

10.4 nM (IC₅₀)

体外研究
(In Vitro)

EGFR-IN-48 (compound 23) (10 nM) shows anti-proliferative activities against BaF3^{EGFR del19/T790M/C797S}and PC-9^{EGFR del19/T790M/C797S}cells with IC₅₀s of 1.526, 66.7 nM, respectively^[1].
EGFR-IN-48 exhibits potent inhibitory activities against various clinically relevant EGFR mutants with IC₅₀s of 10.4, 3.1, 0.9, 0.1, 0.2, 0.3, 0.2 nM for EGFR^WT, EGFR^LR, EGFR^del19, EGFR^del19/TM, EGFR^LR/TM, EGFR^LR/TM/CS, EGFR^drl19/TM/CS, respectively^[1].

Cell Proliferation Assay^[1]

Cell Line:	BaF3^{EGFR del19/T790M/C797S}, PC-9^{EGFR del19/T790M/C797S}cells
Concentration:	10 nM
Incubation Time:
Result:	Showed anti-proliferative activities against BaF3^{EGFR del19/T790M/C797S}and PC-9^{EGFR del19/T790M/C797S}cells with IC₅₀s of 1.526, 66.7 nM, respectively.

体内研究
(In Vivo)

EGFR-IN-48 (2 mg/kg for i.v.; 10 mg/kg for o.p.) shows good oral bioavailability and high plasma exposure in CD-1 mouse^[1].Pharmacokinetic Parameters of EGFR-IN-48 in CD-1 mouse^[1].

Route	Dose (mg/kg)	V_dss(L/kg)	T_1/2(h)	CL (L/h/kg)	AUC_0-last(h*ng/mL)	C_max(ng/mL)	T_max(h)	F (%)
i.v.	2	0.7	3.3	2.4	13820.0
p.o.	10				33811.0	6600.0	0.5	48.9

CD-1 mouse; 2 mg/kg for i.v.; 10 mg/kg for o.p.^[1].

Animal Model:	CD-1 mouse^[1]
Dosage:
Administration:	2 mg/kg for i.v.; 10 mg/kg for o.p.
Result:	Showed good oral bioavailability and high plasma exposure.

分子量

800.75

Formula

C₃₅H₄₇BrN₉O₄PS

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.