2. Protein Tyrosine Kinase/RTK
  3. VEGFR PDGFR
  4. BMS-605541

BMS-605541 is a selective and orally active inhibitor of VEGFR-2 kinase with an IC50 value of 23 nM and Ki value of 49 nM. BMS-605541 inhibits the activity of Flk-1, VEGFR-1 and PDGFR-β with IC50 values of 40 nM, 400 nM and 200 nM, respectively. BMS-605541 can be used for cancer research.

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

BMS-605541 Chemical Structure

BMS-605541 Chemical Structure

CAS No. : 639858-32-5

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5 mg USD 95 In-stock
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50 mg USD 520 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

BMS-605541 Related Antibodies

Top Publications Citing Use of Products

View All VEGFR Isoform Specific Products:

View All Isoforms
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

View All PDGFR Isoform Specific Products:

View All Isoforms
PDGFR PDGFRβ PDGFRα

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BMS-605541 is a selective and orally active inhibitor of VEGFR-2 kinase with an IC50 value of 23 nM and Ki value of 49 nM. BMS-605541 inhibits the activity of Flk-1, VEGFR-1 and PDGFR-β with IC50 values of 40 nM, 400 nM and 200 nM, respectively. BMS-605541 can be used for cancer research[1].

IC50 & Target[1]

VEGFR-2

23 nM (IC50)

VEGFR-2

49 nM (Ki)

Flk-1

40 nM (IC50)

VEGFR-1

400 nM (IC50)

PDGFR-β

200 nM (IC50)

In Vitro

BMS-605541 (Compound 14) inhibits the growth of HUVECs through VEGF with an IC50 value of 25 nM[1].

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

BMS-605541 Related Antibodies
In Vivo

BMS-605541 (12.5-180 mg/kg; once a day or twice a day for 14 days) has anti-tumor activity in thymic mice subcutaneously implanted with L2987 and HCT-116 xenografts[1].
Pharmacokinetic (PK) parameters of BMS-605541[1]

Species Administration manner Dose (mg/kg) Cmax (µM) Tmax (h) AUC (µM•h) T1/2 (h) MRT (h) Cl (mL/min•kg) Vss (L/kg) Fpo (%)
Mouse Oral gavage 90 148 0.5 649 (0-24 h) 1.7 3.4 100
Mouse Intravenous injection 10 11.8 1.7 100
Rat Oral gavage 50 44.0 2.0 202 2.2 3.5 100
Rat Intravenous injection 10 13.6 1.1 100
Cyno Oral gavage 5 8.0 0.75 28.5 7.1 7.9 52
Cyno Intravenous injection 1 3.9 1.6 52

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

401.43

Formula

C19H17F2N5OS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=C(C=C(C(F)=C1)C(NC2CC2)=O)NCC3=CN=C(S3)NC4=NC=CC=C4
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 : 33.33 mg/mL (83.03 mM; ultrasonic and warming and heat to 60°C; 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 2.4911 mL 12.4555 mL 24.9109 mL
5 mM 0.4982 mL 2.4911 mL 4.9822 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
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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: ≥ 2.08 mg/mL (5.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(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 2.4911 mL 12.4555 mL 24.9109 mL 62.2774 mL
5 mM 0.4982 mL 2.4911 mL 4.9822 mL 12.4555 mL
10 mM 0.2491 mL 1.2455 mL 2.4911 mL 6.2277 mL
15 mM 0.1661 mL 0.8304 mL 1.6607 mL 4.1518 mL
20 mM 0.1246 mL 0.6228 mL 1.2455 mL 3.1139 mL
25 mM 0.0996 mL 0.4982 mL 0.9964 mL 2.4911 mL
30 mM 0.0830 mL 0.4152 mL 0.8304 mL 2.0759 mL
40 mM 0.0623 mL 0.3114 mL 0.6228 mL 1.5569 mL
50 mM 0.0498 mL 0.2491 mL 0.4982 mL 1.2455 mL
60 mM 0.0415 mL 0.2076 mL 0.4152 mL 1.0380 mL
80 mM 0.0311 mL 0.1557 mL 0.3114 mL 0.7785 mL
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BMS-605541 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-605541639858-32-5BMS605541BMS 605541VEGFRPDGFRVascular endothelial growth factor receptorPlatelet-derived growth factor receptorRatCynoMouseL2987HCT-116Inhibitorinhibitorinhibit

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