JBJ-09-063 TFA|西域试剂

JBJ-09-063 TFA,99.64%

产品编号：Bellancom-147183A| 分子式：C₃₃H₃₀F₄N₄O₅S| 分子量：670.67

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	包装	价格	库存与货期	购买量	操作
Bellancom-147183A		￥4500.00	杭州北京（现货）
Bellancom-147183A		￥8000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

JBJ-09-063 TFA

产品介绍

JBJ-09-063 TFA 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 TFA 有效降低 EGFR、Akt 和 ERK1/2 磷酸化。JBJ-09-063 TFA 对 EGFR 酪氨酸激酶抑制剂 (TKI) 敏感和耐药模型均有效。JBJ-09-063 TFA 可用于 EGFR 突变型肺癌研究。

生物活性

JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC₅₀s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer.

体外研究

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.
JBJ-09-063 is effective in H1975 cells exogenously expressing the osimertinib-resistant mutations.
JBJ-09-063 exhibits IC₅₀s of 50 nM and 6 nM in Ba/F3 cell when use alone or combination with Cetuximab (HY-P9905).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Mice

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.

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

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Mice

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.

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

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (149.10 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.4910 mL	7.4552 mL	14.9105 mL
5 mM	0.2982 mL	1.4910 mL	2.9821 mL
10 mM	0.1491 mL	0.7455 mL	1.4910 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献