BI-4142

Name: BI-4142
Brand: MedChemExpress
SKU: HY-150024
Rating: 4.5 (1 reviews)

Cat. No.: HY-150024 Purity: 96.48%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC₅₀ of 5 nM.

For research use only. We do not sell to patients.

BI-4142 Chemical Structure

CAS No. : 2682003-36-5

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC₅₀ of 5 nM^[1].

IC₅₀ & Target

HER2

5 nM (IC₅₀)

In Vitro

BI-4142 shows inhibition with IC₅₀ values of 10 nM, 18 nM, 270 nM and 2400 nM against HEK HER2^YVMA, Ba/F3 HER2^YVMA, HEK EGFR^WT and 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^WT and Ba/F3 EGFR^C775S cells
Concentration:	1 nM-5 μM
Incubation Time:	72 h or 96 h
Result:	Showed antiproliferative effect with IC₅₀ values 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^WT and Ba/F3 EGFR^C775S, respectively.

In Vivo

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NMRI-Foxn1nu mice, PC-9 HER2^YVMA xenograft 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 (h•nM)	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

Molecular Weight

521.57

Formula

C₂₈H₂₇N₉O₂

CAS No.

2682003-36-5

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N1CCN(CC1)C2=NC=C3N=CN=C(C3=N2)NC4=CC=C(C(C)=C4)OC5=CC(N=CN6C)=C6C=C5)C=C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (191.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.79 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 96.48%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (247 KB) HNMR (270 KB) RP-HPLC (237 KB)

Handling Instructions (2659 KB)

References

[1]. Wilding B, et al. Discovery of potent and selective HER2 inhibitors with efficacy against HER2 exon 20 insertion-driven tumors, which preserve wild-type EGFR signaling. Nat Cancer. 2022 Jul;3(7):821-836. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9173 mL	9.5864 mL	19.1729 mL	47.9322 mL
	5 mM	0.3835 mL	1.9173 mL	3.8346 mL	9.5864 mL
	10 mM	0.1917 mL	0.9586 mL	1.9173 mL	4.7932 mL
	15 mM	0.1278 mL	0.6391 mL	1.2782 mL	3.1955 mL
	20 mM	0.0959 mL	0.4793 mL	0.9586 mL	2.3966 mL
	25 mM	0.0767 mL	0.3835 mL	0.7669 mL	1.9173 mL
	30 mM	0.0639 mL	0.3195 mL	0.6391 mL	1.5977 mL
	40 mM	0.0479 mL	0.2397 mL	0.4793 mL	1.1983 mL
	50 mM	0.0383 mL	0.1917 mL	0.3835 mL	0.9586 mL
	60 mM	0.0320 mL	0.1598 mL	0.3195 mL	0.7989 mL
	80 mM	0.0240 mL	0.1198 mL	0.2397 mL	0.5992 mL
	100 mM	0.0192 mL	0.0959 mL	0.1917 mL	0.4793 mL

BI-4142 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BI-41422682003-36-5BI4142BI 4142EGFREpidermal growth factor receptorErbB-1HER1HEKBa/F3PC-9antitumorInhibitorinhibitorinhibit

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BI-4142

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BI-4142 Related Antibodies

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Complete Stock Solution Preparation Table

BI-4142 Related Classifications

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