1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. Bcr-Abl
    Apoptosis
  3. S116836

S116836 

Cat. No.: HY-123450 Purity: 99.60%
Handling Instructions

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.

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

S116836 Chemical Structure

S116836 Chemical Structure

CAS No. : 1257628-57-1

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5 mg USD 500 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
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25 mg USD 1800 In-stock
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50 mg USD 3000 In-stock
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100 mg USD 4600 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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].

IC50 & Target[1]

Bcr-AblWT

 

Bcr-AblT315I

 

In Vitro

S116836 (0.01-1 μM; 24 hours) significantly reduces the cellular proliferation of BaF3/WT and BaF3/T315I cells (IC50 values of 0.05 μM and 0.20 μM, respectively)[1].
S116836 (0.01-1 μM; 24 hours) significantly downregulates the expression level of p-BCR-ABL in BaF3/WT cells. S116836 (0.01-1 μM; 24 hours) also significantly downregulates the expression level of p-Crkl and p-STAT5 (downstream signaling proteins of BCR-ABL) in both BaF3/WT and BaF3/T315I cells[1].
S116836 (0.1, 0.3, and 0.5 μM; 24 hours) arrests the BaF3/WT and BaF3/T315I cells in G0/G1 phase of the cell cycle[1].
S116836 (0.3 and 0.5 μM; 24 hours) increases ROS production and decreases GSH levels in BaF3/WT and BaF3/T315I cells[1].
S116836 (0.1, 0.3, and 0.5 μM; 24 hours) induces apoptosis in BaF3/WT and BaF3/T315I cells[1].
S116836 potently inhibits PDGFRα and its downstream signaling molecules such as STAT3, AKT, and Erk1/2. S116836 effectively inhibits the growth of the WT and T674I FIP1L1-PDGFRα-expressing neoplastic cells[3].

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

In Vivo

S116836 (100 or 200 mg/kg; i.p.; q3d×6, athymic NCR nude mice) decreases the volume and weight of xenograft tumors expressing WT and T315I mutant BCR-ABL[1].
S116836 (200mg/kg/d, oral gavage for 14 days) inhibits the growth of xenografted T674I-FIP1L1-PDGFRα cells in nude mice[3].

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

Molecular Weight

502.49

Formula

C27H21F3N6O

CAS No.
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Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 65 mg/mL (129.36 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9901 mL 9.9504 mL 19.9009 mL
5 mM 0.3980 mL 1.9901 mL 3.9802 mL
10 mM 0.1990 mL 0.9950 mL 1.9901 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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S116836
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