JBJ-09-063

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JBJ-09-063

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。

CAS NO:

2820336-67-0

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

JBJ-09-063 是一种突变选择性变构EGFR抑制剂，对 EGFR L858R、EGFR L858R/T790M、EGFR L858R/T790M/C797S 和 EGFRLT/L747S 的IC₅₀分别为 0.147 nM、0.063 nM、0.083 nM 和 0.396 nM。JBJ-09-063 有效降低 EGFR、Akt 和 ERK1/2 磷酸化。JBJ-09-063 对 EGFR 酪氨酸激酶抑制剂 (TKI) 敏感与耐药模型均有效。JBJ-09-063 可用于 EGFR 突变型肺癌研究。

生物活性

JBJ-09-063 is a mutant-selective allostericEGFRinhibitor withIC₅₀s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM forEGFRL858R,EGFRL858R/T790M,EGFRL858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reducesEGFR,Aktand ERK1/2 phosphorylation. JBJ-09-063 is effective acrossEGFRtyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lungcancer^[1].

IC₅₀& Target^[1]

EGFR L858R

0.147 nM (IC₅₀)

EGFR L858R/T790M

0.063 nM (IC₅₀)

EGFR L858R/T790M/C797S

0.083 nM (IC₅₀)

EGFRLT/L747S

0.396 nM (IC₅₀)

体外研究
(In Vitro)

JBJ-09-063 is remarkably effective at inhibiting cell growth and leads to a significant increase in apoptosis, even though H3255GR cells are resistant to gefitinib as a single agent, as they contain an EGFR T790M mutation^[1].
JBJ-09-063 is effective in H1975 cells exogenously expressing the osimertinib-resistant mutations^[1].
JBJ-09-063 exhibits IC₅₀s of 50 nM and 6 nM in Ba/F3 cell when use alone or combination withCetuximab(HY-P9905)^[2].

体内研究
(In Vivo)

JBJ-09-063 (3 mg/kg i.v., 20 mg/kg p.o.) exhibits favorable pharmacokinetics properties and is sufficiently stable to deliver good efficacy upon oral dosing^[2].

Animal Model:

Mice^[2]

Dosage:

3 mg/kg for i.v., 20 mg/kg for p.o.

Administration:

i.v. and p.o.; single dosage

Result:

Pharmacokinetic Parameters of JBJ-09-063 in mice^[2].

Cl (mL/min/kg), i.v.	T_1/2(h)	V_ss(L/kg)	F (%)	AUC 8h (ng·h/mL)
15.7	2.3	2.5	15	2398

分子量

556.65

Formula

C₃₁H₂₉FN₄O₃S

CAS 号

2820336-67-0

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.

溶解性数据

In Vitro:

DMSO : 120 mg/mL(215.58 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	1.7965 mL	8.9823 mL	17.9646 mL
5 mM	0.3593 mL	1.7965 mL	3.5929 mL
10 mM	0.1796 mL	0.8982 mL	1.7965 mL