1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
    VEGFR
  3. BMS-690514

BMS-690514 

Cat. No.: HY-10333 Purity: 99.37%
Handling Instructions

BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR; has IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.

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

BMS-690514 Chemical Structure

BMS-690514 Chemical Structure

CAS No. : 859853-30-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 233 In-stock
Estimated Time of Arrival: December 31
2 mg USD 192 In-stock
Estimated Time of Arrival: December 31
5 mg USD 288 In-stock
Estimated Time of Arrival: December 31
10 mg USD 462 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1188 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Based on 2 publication(s) in Google Scholar

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Description

BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR; has IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.

IC50 & Target[1]

EGFR

5 nM (IC50)

HER2

20 nM (IC50)

HER4

60 nM (IC50)

In Vitro

BMS-690514 targets several critical signaling pathways: human epidermal growth factor receptor (HER)/ErbB, angiogenesis signaling through VEGFR2, lymphangiogenesis through VEGFR3, and also shows activity against VEGFR1, Flt-3, and Lck. Permeability of BMS-690514 in Caco-2 cells is in the intermediate range with a moderate potential to be a P-gp substrate[2]. BMS-690514 inhibits members of the VEGFR family with IC50 values in the range of 25 to 50 nM. Non–small cell lung tumor cells with exon 19 deletion (HCC4006, HCC827, and PC9) are highly sensitive to BMS-690514, which inhibits their proliferation with IC50 values of 2 to 35 nM. Tumor cell lines with EGFR gene amplification (DiFi, NCI-H2073, A431) are also highly sensitive to inhibition by BMS-690514. Tumor cell lines that are dependent on HER2 signaling are also found to be highly sensitive to BMS-690514. Breast and gastric tumor cell lines that have HER2 gene amplification (N87, SNU-216, AU565, BT474, KPL4, and HCC202) are inhibited with IC50 values of 20 to 60 nM[1].

In Vivo

BMS-690514 has been shown to be efficacious in a broad spectrum of tumor xenografts. At doses that are efficacious and well tolerated in the animal models, BMS-690514 inhibits tumor cell proliferation and tumor blood flow[1]. The oral bioavailability of BMS-690514 is 78% in mice, 100% in rats, 8% in monkeys, and 29% in dogs. BMS-690514 is able to cross the blood–brain barrier with a brain-to-plasma ratio of 1. The preclinical ADME properties of BMS-690514 suggest good oral bioavailability in humans and metabolism by multiple pathways including oxidation and glucuronidation[2].

Clinical Trial
Molecular Weight

368.43

Formula

C₁₉H₂₄N₆O₂

CAS No.

859853-30-8

SMILES

O[[email protected]@H]1CN(CC[[email protected]]1N)CC2=C3C(NC4=CC=CC(OC)=C4)=NC=NN3C=C2

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 : ≥ 25 mg/mL (67.86 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7142 mL 13.5711 mL 27.1422 mL
5 mM 0.5428 mL 2.7142 mL 5.4284 mL
10 mM 0.2714 mL 1.3571 mL 2.7142 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.79 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.79 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.79 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2]

Rats: BMS-690514 is administered to male Sprague–Dawley rats as a 10 min infusion intraarterially (IA) (1 mg/kg) or orally by gavage (10mg/kg). Vehicles used for dosing are: IA, 10mM acetate buffer (pH 5.0, 1 mL/kg) and PO, PEG400/10mM acetate buffer (pH 5.0, 2 mL/kg) (10:90). Serial plasma samples are obtained predose and at 0.17 (or 0.25 for PO), 0.5, 0.75, 1, 2, 4, 6, 8, 12, and 24 h postdose. Rats are fasted overnight and fed 4 h postdose. The brain uptake of BMS-690514 is investigated after the last dose in a 2-week toxicology study (3, 10, and 30 mg/kg/day). Brain samples are weighed and homogenized in 3 volumes of ice-chilled water. Concentrations of BMS-690514 in plasma and brain homogenates are determined by LC/MS/MS[2].

Mice: The pharmacokinetics of BMS-690514 is investigated in male balb-c mice. A total of 18 mice are divided into two groups to receive BMS-690514 as a single dose of 1mg/kg IV bolus or 5 mg/kg orally by gavage. The vehicle used for both IV (0.1mL/mouse) and PO (0.2mL/mouse) dose is Tween-80/PG/water (10:40:50). Serum concentrations of BMS-690514 are measured at 0.05 (or 0.25 for PO), 0.5, 1, 3, 6, 8, and 24 h postdose. The mice are fasted overnight and fed 6 h after dosing. Three blood samples are taken from each mouse by retro-orbital bleeding and there are three mice per time point. At the 24h time point only one sample is taken from each of the three mice. Composite serum concentration–time profiles are constructed for pharmacokinetic analysis[2].

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

References
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BMS-690514
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