TG101209

SKU: orb1304575

Description

TG101209 is a potent and selective JAK2 inhibitor, demonstrating an IC50 of 6 nM. It is a valuable research tool for studying JAK-STAT signaling in myeloproliferative disease models, both in cellular assays and in vivo studies.

Research Area

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

Key Properties

• CAS Number: 936091-14-4
• MW: 509.67
• Purity: >99.99% (May vary between batches)
• Formula: C₂₆H₃₅N₇O₂S
• SMILES: CN1CCN(CC1)c1ccc(Nc2ncc(C)c(Nc3cccc(c3)S(=O)(=O)NC(C)(C)C)n2)cc1
• Target: Apoptosis,Autophagy,FLT,JAK,c-RET
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.47 mM);DMSO:94 mg/mL (184.43 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  JAK2:6 nM|FLT3:25 nM|JAK3:169 nM|RET:17 nM
• In Vivo:
  TG101209 inhibits survivin in HCC2429 and H460 lung cancer cells and reduces the phosphorylation of STAT3. It induces cell cycle arrest and apoptosis in acute myeloid leukemia cell lines expressing the human JAK2V617F mutation, while inhibiting the phosphorylation of JAK2V617F, STAT5, and STAT3. TG101209 suppresses the growth of Ba/F3 cells expressing the JAK2V617F or MPLW515L mutations, with an IC50 of approximately 200 nM. It inhibits the growth of hematopoietic colonies from progenitors carrying the JAK2V617F or MPL515 mutations. TG101209 significantly reduces the phosphorylation of STAT5 without affecting the total STAT5 protein level. It eliminates the phosphorylation of BCR-JAK2 and STAT5, reduces Bcl-xL expression, and induces apoptosis in transformed Ba/F3 cells.
• In Vitro:
  Compared to animals treated with a placebo, those administered TG101209 exhibited a significant reduction in the burden of circulating tumor cells in a dose-dependent manner, with a reduction ratio of up to 20% at +11 days. Administering 100 mg/kg of TG101209 effectively extended the survival time of animals afflicted with JAK2V617F-induced disease by 10 days.
• Cell Research:
  In brief, approximately 2 × 103 cells are plated into microtiterplate wells in 100 ml RPMI-1640 growth media with indicated concentrations of TG101209. The relative growth of cells is quantified at 24-hour intervals using Cell Proliferation Kit II (XTT) as per manufacturer's guidelines. After incubation, 20 mL of XTT is added to the wells and allowed to incubate for 4-6 hours. The colored formazan product is measured spectrophotometrically at 450 nm with correction at 650 nm, and IC50 values are determined using the GraphPad Prism 4.0 software. Data are subjected to a non-linear regression-fit analysis and IC50 values are determined as the concentration that inhibited proliferation by 50%. All experiments are done in triplicate and the results normalized to growth of untreated cells.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Autophagy, Apoptosis, CD135, Cluster of differentiation antigen 135, cRET, JAK, Janus kinase, JAK3, JAK2, inhibit, Inhibitor, FLT3, Fms like tyrosine kinase 3, RET, TG101209, TG-101209, TG 101209

Compound Identifiers

PubChem CID

16722832