2. MAPK/ERK Pathway Protein Tyrosine Kinase/RTK Membrane Transporter/Ion Channel Cell Cycle/DNA Damage Apoptosis
  3. Raf Bcr-Abl P-glycoprotein PERK Apoptosis
  4. BRAFV600E/ABL2-IN-1

BRAFV600E/ABL2-IN-1 is a BRAFV600E (IC50 = 0.088 μM)/ABL2 (IC50 = 0.3 μM) dual inhibitor. BRAFV600E/ABL2-IN-1 can diminish P-glycoprotein expression. BRAFV600E/ABL2-IN-1 effectively inhibits p-CrkL (Abl2 signaling) and p-ERK1/2 (BRAFV600E pathway) in A375-R melanoma cells. BRAFV600E/ABL2-IN-1 causes cell cycle arrest. BRAFV600E/ABL2-IN-1 significantly increases the percentage of late apoptotic cells. BRAFV600E/ABL2-IN-1 can be used for the study of melanoma.

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

BRAFV600E/ABL2-IN-1

BRAFV600E/ABL2-IN-1 Chemical Structure

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BRAFV600E/ABL2-IN-1 Related Antibodies

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Description

BRAFV600E/ABL2-IN-1 is a BRAFV600E (IC50 = 0.088 μM)/ABL2 (IC50 = 0.3 μM) dual inhibitor. BRAFV600E/ABL2-IN-1 can diminish P-glycoprotein expression. BRAFV600E/ABL2-IN-1 effectively inhibits p-CrkL (Abl2 signaling) and p-ERK1/2 (BRAFV600E pathway) in A375-R melanoma cells. BRAFV600E/ABL2-IN-1 causes cell cycle arrest. BRAFV600E/ABL2-IN-1 significantly increases the percentage of late apoptotic cells. BRAFV600E/ABL2-IN-1 can be used for the study of melanoma[1].

IC50 & Target[1]

BRafV600E

0.088 μM (IC50)

In Vitro

BRAFV600E/ABL2-IN-1 (Compound 8h) (0.01-100 μM, 48 h) exhibits the best activity towards SK-MEL5 cells at the melanoma panel, with a GI50 of 0.54 μM, demonstrating marked cytostatic activity against melanoma (SK-MEL-5; TGI = 19.95 μM) and colon cancer (HT29; TGI = 26.30 μM)[1].
BRAFV600E/ABL2-IN-1 (0.125-1 μM, 72 h) significantly downregulates P-gp expression in SK-MEL-5 cells[1].
BRAFV600E/ABL2-IN-1 (0.4-100 μM) demonstrates IC50 values of 6.888 μg/mL (~12.3 μM) in A375 cells (BRAFV600E mutant) and 11.242 μg/mL (~20.1 μM) in A375-R cells (vemurafenib-resistant), and 28.776 μM in WI-38 cells[1].
BRAFV600E/ABL2-IN-1 significantly reduces the phosphorylation levels of p-CrkL (downstream of ABL2) and p-ERK1/2 (downstream of BRAF), while total protein remains unchanged. p-CrkL decreases by 67.7%, and p-ERK1/2 decreases by 63.0% in A375- R cells[1].
BRAFV600E/ABL2-IN-1 (0.54 μM, 48 h) inhibits cell proliferation in SK-MEL-5 cells by inducing G1 phase arrest and apoptosis[1].

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

BRAFV600E/ABL2-IN-1 Related Antibodies

Real Time qPCR[1]

Cell Line: SK-MEL-5 cells
Concentration: 0.125 μM, 0.25 μM, 0.5 μM, 1 μM
Incubation Time: 72 h
Result: Showed approximately 67.4 % downregulation of P-gp expression in SK-MEL-5 cells.

Cell Cycle Analysis[1]

Cell Line: SK-MEL-5 cells
Concentration: 0.54 μM
Incubation Time: 48 h
Result: Caused G0-G1 phase arrest (58.12% vs. control 44.63%), and reduced S and G2/M phases.

Apoptosis Analysis[1]

Cell Line: SK-MEL-5 cells
Concentration: 0.54 μM
Incubation Time: 48 h
Result: Increased early apoptosis (25.61% vs. control 0.33%) and late apoptosis (13.89% vs. control 0.15%).
Molecular Weight

559.86

Formula

C24H20BrClN4O3S
SMILES

O=C(N/N=C(C1=CC=C(Br)C=C1)\C)CN2C(C3=CC=C(S(=O)(C)=O)C=C3)=NC4=CC(Cl)=CC=C24
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BRAFV600E/ABL2-IN-1 Related Classifications

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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:

BRAFV600E/ABL2-IN-1RafBcr-AblP-glycoproteinPERKApoptosisRaf kinasesP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Protein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseBenzimidazolesBRAFV600EABL2Inhibitorinhibitorinhibit

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