BMS-599626
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.
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- Pureza: 98.56%
- No. CAS: 714971-09-2
- Fòrmula: C27H27FN8O3
- Peso molecular:530.55
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) BMS-599626
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
>10000 nM
Compound: 13, BMS-599626
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Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay
Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay
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[PMID: 19821562] |
| BT-474 | IC50 |
310 nM
Compound: 13, BMS-599626
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Antiproliferative activity against human BT474 cells after 72 hrs by MTT assay
Antiproliferative activity against human BT474 cells after 72 hrs by MTT assay
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[PMID: 19821562] |
| HEK293 | IC50 |
4 μM
Compound: 13, BMS-599626
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Inhibition of human ERG expressed in HEK cells
Inhibition of human ERG expressed in HEK cells
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[PMID: 19821562] |
| NCI-N87 | IC50 |
450 nM
Compound: 13, BMS-599626
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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
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[PMID: 19821562] |
| NCI-N87 | IC50 |
0.45 μM
Compound: 1, BMS-599626
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Antiproliferative activity against human NCI-N87 cells
Antiproliferative activity against human NCI-N87 cells
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[PMID: 21177105] |
| Sf9 | IC50 |
190 nM
Compound: 13, BMS-599626
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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
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[PMID: 19821562] |
| Sf9 | IC50 |
22 nM
Compound: 13, BMS-599626
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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
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[PMID: 19821562] |
| Sf9 | IC50 |
32 nM
Compound: 13, BMS-599626
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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
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[PMID: 19821562] |
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.
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.
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Animal Model:Athymic female nude mice (nu/nu mice, Sal2 tumor model)[1]
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Dosage:60, 120, 240 mg/kg
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Administration:Oral; daily for 14 days
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Result:Resulted in a dose-dependent inhibition of Sal2 tumor growth.
Chemical Information
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No. CAS 714971-09-2
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Appearance Solid
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Peso molecular 530.55
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Fòrmula C27H27FN8O3
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Color White to off-white
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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
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Synonyms
AC480
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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
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Most Recent
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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
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (276 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
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. 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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