Cat. No.: HY-10251

BMS-599626

(Synonyms: AC480)

3 Cited Publications

Customer Review

Based on 3 publication(s) in Google Scholar

BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC₅₀s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC₅₀=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.

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

Purity: 98.56%
CAS No.: 714971-09-2
Formula: C₂₇H₂₇FN₈O₃
Molecular Weight:530.55

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

BMS-599626 Chemical Structure

CAS No.: 714971-09-2

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	>10000 nM Compound: 13, BMS-599626	Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay	[PMID: 19821562]
BT-474	IC₅₀	310 nM Compound: 13, BMS-599626	Antiproliferative activity against human BT474 cells after 72 hrs by MTT assay Antiproliferative activity against human BT474 cells after 72 hrs by MTT assay	[PMID: 19821562]
HEK293	IC₅₀	4 μM Compound: 13, BMS-599626	Inhibition of human ERG expressed in HEK cells Inhibition of human ERG expressed in HEK cells	[PMID: 19821562]
NCI-N87	IC₅₀	450 nM Compound: 13, BMS-599626	Antiproliferative activity against human NCI-N87 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-N87 cells after 72 hrs by MTT assay	[PMID: 19821562]
NCI-N87	IC₅₀	0.45 μM Compound: 1, BMS-599626	Antiproliferative activity against human NCI-N87 cells Antiproliferative activity against human NCI-N87 cells	[PMID: 21177105]
Sf9	IC₅₀	190 nM Compound: 13, BMS-599626	Inhibition of human recombinant HER4 expressed in Sf9 cells by liquid scintillation counting Inhibition of human recombinant HER4 expressed in Sf9 cells by liquid scintillation counting	[PMID: 19821562]
Sf9	IC₅₀	22 nM Compound: 13, BMS-599626	Inhibition of human recombinant HER2 expressed in Sf9 cells by liquid scintillation counting Inhibition of human recombinant HER2 expressed in Sf9 cells by liquid scintillation counting	[PMID: 19821562]
Sf9	IC₅₀	32 nM Compound: 13, BMS-599626	Inhibition of human recombinant HER1 expressed in Sf9 cells by liquid scintillation counting Inhibition of human recombinant HER1 expressed in Sf9 cells by liquid scintillation counting	[PMID: 19821562]

In Vitro

BMS-599626 inhibits the proliferation of tumor cells that are dependent on HER1/HER2 signaling. BMS-599626 (0.03-8 μM; 1 huors) results in the inhibition of receptor autophosphorylation, as well as MAPK phosphorylation, with IC₅₀s of 0.3 and 0.22 μM, respectively, in Sal2 cells which express a CD8HER2 fusion protein^[1].
BMS-599626 abrogates HER1 and HER2 signaling and inhibited the proliferation of tumor cell lines that are dependent on these receptors, with IC₅₀ in the range of 0.24 to 1 μM.In GEO cells, HER1 phosphorylation is stimulated by treatment with EGF and is inhibited by BMS-599626 (IC₅₀=0. 75 μM).There is also nearly complete inhibition of EGF-dependent MAPK (0. 8 μM) but only partial inhibition of AKT signaling.The latter likely reflects the activation of AKT by multiple upstream signals.Treatment of N87 cells with BMS-599626 leads to the inhibition of HER2 (0. 38 μM), which is expressed to a high level because of gene amplification, as well as MAPK and AKT phosphorylation (0.35 μM for both)^[1].
At the molecular level, in HN-5 cells the agent inhibited the expression of pEGFR, pHER2, cyclins D and E, pRb, pAkt, pMAPK, pCDK1 and 2, CDK 6, and Ku70 proteins. The drug also induced accumulation of cells in the G1 cell cycle phase, inhibited cell growth, enhanced radiosensitivity, and prolonged the presence of γ-H AX foci up to 24 h after radiation^[2].

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

In Vivo

BMS-599626 (60-240 mg/kg; p.o.; daily for 14 days) results in a dose-dependent inhibition of Sal2 tumor growth^[1].
BMS599626 treatment results in the inhibition of GEO xenograft tumor growth when given once daily for 14 days. In addition to efficacy in the Sal2, GEO, and KPL4 models, BMS-599626 has similar antitumor activity in other HER2 amplified xenograft models including the BT474 breast and N87 gastric tumors, as well as other HER1-overexpressing non-small-cell lung tumors (A549 and L2987)^[1].
BMS599626 given before and during irradiation improved the radioresponse of HN5 tumors in vivo^[2].

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

Animal Model:

Athymic female nude mice (nu/nu mice, Sal2 tumor model)^[1]
Dosage:

60, 120, 240 mg/kg
Administration:

Oral; daily for 14 days
Result:

Resulted in a dose-dependent inhibition of Sal2 tumor growth.

Chemical Information

CAS No. 714971-09-2
Appearance Solid
Molecular Weight 530.55
Formula C₂₇H₂₇FN₈O₃
Color White to off-white
SMILES

O=C(NC1=CN2C(C(NC3=CC4=C(N(CC5=CC=CC(F)=C5)N=C4)C=C3)=NC=N2)=C1C)OC[C@H]6NCCOC6
Synonyms

AC480
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (3)

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Journal Impact Factor

Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Life Sci

Skp2 promotes APL progression through the stabilization of oncoprotein PML-RARα and the inhibition of JunB expression. [Abstract]

2021 Dec 16;289:120231. PMID: 34921867
BMC Pulm Med

The combination therapy of isomucronulatol 7-O-beta-glucoside (IMG) and CEP-9722 targeting ferroptosis-related biomarkers in non-small cell lung cancer (NSCLC). [Abstract]

2023 May 11;23(1):162. PMID: 37165402

Solvent & Solubility

In Vitro:

DMSO : 110 mg/mL (207.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8848 mL

9.4242 mL

18.8484 mL

5 mM

0.3770 mL

1.8848 mL

3.7697 mL

10 mM

0.1885 mL

0.9424 mL

1.8848 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

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Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.75 mg/mL (5.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.75 mg/mL (5.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.75 mg/mL (5.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Wong TW, et al. Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling. Clin Cancer Res. 2006 Oct 15;12(20 Pt 1):6186-93. [Content Brief]

[2]. Torres MA, et al. AC480, formerly BMS-599626, a pan Her inhibitor, enhances radiosensitivity and radioresponse of head and neck squamous cell carcinoma cells in vitro and in vivo. Invest New Drugs. 2011 Aug;29(4):554-61. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8848 mL	9.4242 mL	18.8484 mL	47.1209 mL
	5 mM	0.3770 mL	1.8848 mL	3.7697 mL	9.4242 mL
	10 mM	0.1885 mL	0.9424 mL	1.8848 mL	4.7121 mL
	15 mM	0.1257 mL	0.6283 mL	1.2566 mL	3.1414 mL
	20 mM	0.0942 mL	0.4712 mL	0.9424 mL	2.3560 mL
	25 mM	0.0754 mL	0.3770 mL	0.7539 mL	1.8848 mL
	30 mM	0.0628 mL	0.3141 mL	0.6283 mL	1.5707 mL
	40 mM	0.0471 mL	0.2356 mL	0.4712 mL	1.1780 mL
	50 mM	0.0377 mL	0.1885 mL	0.3770 mL	0.9424 mL
	60 mM	0.0314 mL	0.1571 mL	0.3141 mL	0.7853 mL
	80 mM	0.0236 mL	0.1178 mL	0.2356 mL	0.5890 mL
	100 mM	0.0188 mL	0.0942 mL	0.1885 mL	0.4712 mL

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BMS-599626

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Publications Citing Use of MedChemExpress (MCE) BMS-599626

All EGFR Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

BMS-599626 Related Classifications

HY-10251 Related Classifications