2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. BMS-599626

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.

BMS-599626

BMS-599626 Chemical Structure

CAS No. : 714971-09-2

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Based on 3 publication(s) in Google Scholar

Other Forms of BMS-599626:

BMS-599626 Related Antibodies

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

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]
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]
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.

BMS-599626 Related Antibodies
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.
Clinical Trial
Molecular Weight

530.55

Formula

C27H27FN8O3
CAS No.
Appearance

Solid

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
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
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8848 mL 9.4242 mL 18.8484 mL
5 mM 0.3770 mL 1.8848 mL 3.7697 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. 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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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: ≥ 2.75 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.
  • 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.

    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

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(per animal)

g

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).
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
References

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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BMS-599626 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:

BMS-599626714971-09-2AC480BMS599626BMS 599626AC 480AC-480EGFREpidermal growth factor receptorErbB-1HER1antitumorselectiveproliferationcancer autophosphorylationGEOKPL4Sal2cellsInhibitorinhibitorinhibit

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