BI-4142

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BI-4142

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:

2682003-36-5

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议

产品介绍

BI-4142 是一种有效的、高选择性的、具有口服活性的HER2抑制剂，IC₅₀值为 5 nM。

生物活性

BI-4142 is a potent, highly selective and orally activeHER2inhibitor with anIC₅₀of 5 nM^[1].

IC₅₀& Target

HER2

5 nM (IC₅₀)

体外研究
(In Vitro)

BI-4142 shows inhibition with IC₅₀values of 10 nM, 18 nM, 270 nM and 2400 nM against HEK HER2^YVMA, Ba/F3 HER2^YVMA, HEK EGFR^WTand Ba/F3 EGFR^WT, respectively^[1].
BI-4142 (1 nM-5 μM, 72 h or 96 h) shows antiproliferative activity against tumor cells^[1].
BI-4142 displays good permeability and no PgP-mediated efflux liability in the CaCo-2 assay^[1].
BI-4142 inhibits HER2-dependent cell lines and inhibits downstream signaling^[1].

Cell Proliferation Assay^[1]

Cell Line:	NCI-H2170 HER2^WT, NCI-H2170 HER2^YVMA, A431 EGFR^WT, Ba/F3 HER2^YVMA, Ba/F3 HER2^YVMA,S783C, Ba/F3 EGFR^WTand Ba/F3 EGFR^C775Scells
Concentration:	1 nM-5 μM
Incubation Time:	72 h or 96 h
Result:	Showed antiproliferative effect with IC₅₀values of 16 nM, 82 nM, >5 μM, 4 nM, 24 nM, 718 nM and 43 nM against NCI-H2170 HER2^WT, NCI-H2170 HER2^YVMA, A431 EGFR^WT, Ba/F3 HER2^YVMA, Ba/F3 HER2^YVMA,S783C, Ba/F3 EGFR^WTand Ba/F3 EGFR^C775S, respectively.

体内研究
(In Vivo)

BI-4142 (0-100 mg/kg; p.o.; twice per day for 40 days) inhibits tumor growth and inhibits oncogenic signaling^[1].

Animal Model:	NMRI-Foxn1nu mice, PC-9 HER2^YVMAxenograft model^[1]
Dosage:	3, 10, 30 and 100 mg/kg
Administration:	Oral administration, twice per day for 40 days
Result:	Resulted in tumor regressions in a dose-dependent manner (113%, 126%, 153% and 166% tumor growth inhibition at 3, 10, 30 and 100 mg/kg, respectively).

Animal Model:

BomTac:NMRI Foxn1nu mice^[1]

Dosage:

1 mg/kg or 10mg/kg and 100 mg/kg

Administration:

IV for 1 mg/kg, PO for 10mg/kg and 100 mg/kg (Pharmacokinetic Analysis)

Result:

In vivo mouse PK data for BI-4142^[1]

Compound	Dose iv/po (mg/kg)	tmax (h)	C_max (nM)	AUD (honM)	Plasma CL (mL/min/kg)	% F
	i.v., 1mg/kg	n/a	n/a	3,280	9.69	n/a
BI-4142	p.o., 10 mg/kg	0.83	8,600	23,200	n/a	71
	p.o., 100 mg/kg	0.67	36,400	196,000	n/a	60

分子量

521.57

性状

Solid

Formula

C₂₈H₂₇N₉O₂

CAS 号

2682003-36-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : 100 mg/mL(191.73 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	1.9173 mL	9.5864 mL	19.1729 mL
5 mM	0.3835 mL	1.9173 mL	3.8346 mL
10 mM	0.1917 mL	0.9586 mL	1.9173 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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。