Fig. 1 · Structure

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Brivanib (BMS-540215)

Cat. No. A10254 CAS 649735-46-6

VEGFR-2 inhibitor

Brivanib (BMS-540215) is a VEGFR -2 inhibitor with an IC50 of 25 nM and Ki of 26 nM.

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Publications for Brivanib

2 publications citing this product

  1. Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
  2. Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168

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Biological Activity

Target & Activity

Target Activity Value
VEGFR2 IC50 25nM
Flk1 IC50 89nM
FGFR1 IC50 148nM
VEGFR1 IC50 380nM
EGFR IC50 >1.9μM
LCK IC50 >2.5μM
PDGFRβ IC50 >6μM
PKCα IC50 >25μM
JAK3 IC50 >50μM

9 targets · Scroll to view more

In Vitro Studies

Brivanib showed model-dependent responses in an endometrial cancer screening assay. The plotted growth-response AUC was higher in RL95-2 cells than in REME9 and REME16 patient-derived organoids or AN3 CA cells, consistent with weaker growth inhibition in RL95-2 under the tested conditions. These ATP-based screening results do not establish direct VEGFR/FGFR target inhibition or a clinical response. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Brivanib response in endometrial organoids and cell lines

Cell-based study · REME9 and REME16 endometrial cancer patient-derived organoids; AN3 CA and RL95-2 endometrial cancer cell lines [1]

One comparative drug-screen design, represented once across all four models. Figure 6 shows the highest brivanib growth-response AUC in RL95-2, indicating a weaker inhibitory response than in the other plotted models; this is a qualitative visual comparison, without numerical bar extraction.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Area under the ATP-based growth-response curve, qualitatively compared across the four model columnsGrowth-response AUC (qualitative) RL95-2 > REME9, REME16 and AN3 CA (visual comparison; exact AUC values not extracted)[1]

Literature-Reported Treatment Conditions

Treatment concentration
Serial concentrations up to 20 µM; lower-bound discrepancy retained in missing information.
Exposure duration
144 h after treatment in the shared 384-well assay methods
Method
Single-agent comparative growth-response screen in 384-well plates
Vehicle
DMSO vehicle control; shared assay methods specify maximum 0.1%.
Reported limits
Methods specify ten concentrations from 1.0 nM to 20 µM; Figure 6 caption instead states 0.1–20 µM. The lower bound is unresolved and omitted from public interpretation. Exact model-specific AUC values, raw replicate data, lot number and stereochemical verification are not supplied in the reviewed locations.
Methods and source locations

Compound reported in the paper: Brivanib; Compound label in the paper: Brivanib (Table II)

Response of the material named brivanib in this experiment only; no alaninate conversion or quantitative kinase potency inference.

Figure 6 (brivanib row, all four model columns); Table II (Brivanib row); Materials and methods: Compounds, Cell culture, Growth inhibition assays using multi-well plates

Area under the ATP-based growth-response curve, qualitatively compared across the four model columns: CellTiter-Glo 3D ATP readout; response normalized to vehicle control after background subtraction; AUC calculated with Morphit 5.0. Figure 6 reports means of triplicate experiments; no error bars or between-model statistical test shown. — Figure 6, brivanib row and caption; Growth inhibition assays using multi-well plates

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 649735-46-6
Applications VEGFR-2 inhibitor
Formula C19H19FN4O3
Molecular Weight 370.4
Synonyms BMS-540215
SMILES
CC1=CC2=C(N1)C=CC(=C2F)OC3=NC=NN4C3=C(C(=C4)OC[C@@H](C)O)C

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 71 mg/mL (191.69 mM)
Water Insoluble
Ethanol 3 mg/mL (8.09 mM)

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Tamura H, Higa A, Hoshi H, et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues. Oncology Reports (2018). PMID: 29917168 DOI: 10.3892/or.2018.6501 Source material

Publications

2 publications citing this product

  1. Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
  2. Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168

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