EGFR-IN-48 | 赛默飞Alfa aesar官网

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EGFR-IN-48

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。

EGFR-IN-48 Chemical Structure

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

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生物活性

EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC₅₀s of 0.193 nM, 0.251 nM, 10.4 nM for EGFR^d19/TM/CS, EGFR^LR/TM/CS, EGFR^WT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3^{EGFR del19/T790M/C797S} and PC-9^{EGFR del19/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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

参考文献

[1]. Fang H, et al. Design, synthesis and evaluation of the Brigatinib analogues as potent inhibitors against tertiary EGFR mutants (EGFRdel19/T790M/C797S and EGFRL858R/T790M/C797S). Bioorg Med Chem Lett. 2022; 9:128729.

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