S116836

S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies[1][2][3]. S116836 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Product Specifications

CAS Number

[1257628-57-1]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Bcr-Abl; PDGFR

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/s116836.html

Purity

99.78

Solubility

DMSO : 32 mg/mL (ultrasonic; warming; heat to 80°C)

Smiles

O=C(C1=CC=C(C(C#CC2=CN=C(N=C2)NC3CC3)=C1)C)NC4=CC(C(F)(F)F)=CC(N5C=CN=C5)=C4

Molecular Formula

C27H21F3N6O

Molecular Weight

502.49

Precautions

H302, H315, H319, H335

References & Citations

[1]Gupta P, et al. Preclinical development of a novel BCR-ABL T315I inhibitor against chronic myeloid leukemia. Cancer Lett. 2020;472:132-141. |[2]Bu Q, et al. SAHA and S116836, a novel tyrosine kinase inhibitor, synergistically induce apoptosis in imatinib-resistant chronic myelogenous leukemia cells. Cancer Biol Ther. 2014;15 (7) :951-962. |[3]Shen Y, et al. Antitumor activity of S116836, a novel tyrosine kinase inhibitor, against imatinib-resistant FIP1L1-PDGFRα-expressing cells. Oncotarget. 2014;5 (21) :10407-10420.