[CAS NO. 936091-14-4] TG101209
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PRODUCTS SPECIFICATIONS [936091-14-4]
Catalog
SLK-S2692
Brand
Selleck
CAS
936091-14-4
DESCRIPTION [936091-14-4]
Overview
| MDL | MFCD15528085 |
|---|---|
| Molecular Weight | 509.67 |
| Molecular Formula | C26H35N7O2S |
| SMILES | O=S(C1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3)=NC=C2C)=C1)(NC(C)(C)C)=O |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9621 mL | 9.8103 mL | 19.6205 mL |
| 5 mM | 0.3924 mL | 1.9621 mL | 3.9241 mL |
| 10 mM | 0.1962 mL | 0.9810 mL | 1.9621 mL |
| 50 mM | 0.0392 mL | 0.1962 mL | 0.3924 mL |
Description
TG101209 is a selective inhibitor with of 6 nM, less potent to Flt3 and RET (c-RET) with of 25 nM and 17 nM in cell-free assays, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations.
Targets
In vitro
TG101209 is an orally bioavailable, small molecule, ATP-competitive inhibitor towards several tyrosine kinases. TG101209 inhibits growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with an IC50 of B200 nM. In a human JAK2V617F-expressing acute myeloid leukemia cell line, TG101209 inducs cell cycle arrest and apoptosis, and inhibits phosphorylation of JAK2V617F, STAT5 and STAT3. TG101209 suppresses growth of hematopoietic colonies from primary progenitor cells harboring JAK2V617F or MPL515 mutations.
TG101209 significantly reduces STAT5 phosphorylation without affecting the total amount of STAT5 protein.
TG101209 inhibits survivin and reduces phosphorylation of STAT3 in HCC2429 and H460 lung cancer cells. TG101209 results in radio sensitization of HCC2429 and H460 lung cancer cells in vitro. A recent study indicates TG101209 abrogates BCR-JAK2 and STAT5 phosphorylation, decreases Bcl-xL expression and triggered apoptosis of transformed Ba/F3 cells.
In vivo
100 mg/kg of TG101209 effectively prolongs the survival in JAK2V617F-induced disease (10 days). Compared with placebo-treated animals, TG101209-treated animals exhibit statistically significant, dose-dependent reduction in the circulating tumor cell burden at day +11 to 20%.
References
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