SB1317

SKU: orb1701281

Description

SB1317 (TG02) is a multi-kinase inhibitor that potently targets CDKs, JAK2, and FLT3. It is a valuable research tool for studying oncology and hematological malignancies, with demonstrated activity in both in vitro cellular assays and in vivo preclinical models of cancer.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1204918-72-8
• MW: 372.46
• Purity: >99.99% (May vary between batches)
• Formula: C₂₃H₂₄N₄O
• SMILES: CN1C\C=C\CCOc2cccc(c2)C2=CC=N\C(N2)=N\c2cccc(C1)c2
• Target: CDK,JAK,FLT
• Solubility: DMSO:10 mM;10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.37 mM)

Bioactivity

• In Vitro:
  SB1317 has a highly novel kinase inhibitory spectrum inhibiting 17 kinases from a panel of 63, 11 of which are CDK/JAK/FLT family members. The others, Lck, Fyn, Fms, TYRO3, ERK5, and p38δ, are implicated in inflammatory and proliferative processes. Human CYP1A2, 3A4, 2C9, and 2C19 isoforms are not inhibited by SB1317 at the highest tested concentration of 25 μM, but SB1317 inhibits CYP2D6 with IC50=0.95 μM, approximately at the plasma Cmax observed at the maximum tolerated dose. SB1317 inhibits cell proliferation concentrations in HCT-116 (IC50=0.079 μM) and HL-60 (IC50=0.059 μM). SB1317 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor. SB1317 is mainly metabolized by CYP3A4 and CY1A2 in vitro. SB1317 does not inhibit any of the major human CYPs in vitro except CYP2D6 (IC50=1 μM). SB1317 does not significantly induce CYP1A and CYP3A4 in human hepatocytes in vitro.
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• Cell Research:
  SB1317 is prepared in DMSO and stored, and then diluted with appropriate medium before use. All cell lines are obtained from the American Type Culture Collection and cultured. For proliferation assays in 96-well plates, 20 000 cells are seeded in 100 μL of medium and treated the following day with compounds (e.g., SB1317 ) (in triplicate) at concentrations up to 10 μM for 48 h. Cell viability is monitored using the CellTiter-96 Aqueous One solution cell proliferation assay. Dose-response curves are plotted to determine IC50 values for the compounds using the XL-fit software.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

JAK2, JAK, FLT3, CDKs, CDK, TG02, TG-02, TG 02, SB1317, SB-1317, SB 1317

Compound Identifiers

PubChem CID

16739650