EGFR-IN-48 | whatman (沃特曼)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

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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