CS-94
TG101209
CAS: 936091-14-4
Molecular Formula: C26H35N7O2S
CS-94 - Names and Identifiers
CS-94 - Physico-chemical Properties
| Molecular Formula | C26H35N7O2S |
| Molar Mass | 509.67 |
| Density | 1.250 |
| Melting Point | 243 °C |
| Boling Point | 703.1±70.0 °C(Predicted) |
| pKa | 11.95±0.50(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | 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 sensitivity of HCC2429 and H460 lung cancer cells in vitro. A recent study invasive TG101209 abrogates BCR-JAK2 and STAT5 phosphation, malignant Bcl-xL expression and trigged apoptosis of transformed Ba/F3 cells. TG101209 is an orally bioavailable, small-molecule, ATP-competitive inhibitor of several tyrosine kinases. TG101209 inhibited the growth of Ba/F3 cells expressing JAK2V617F or mpw515l mutants with an IC50 of B200 nM. In acute myeloid leukemia cell lines expressing human JAK2V617F, TG101209 induces cell cycle arrest and apoptosis, and inhibits JAK2V617F,STAT5 and STAT3 phosphorylation. TG101209 inhibited the growth of hematopoietic colonies in primary progenitor cells from JAK2V617F or MPL 515 mutants. TG101209 significantly reduced STAT5 phosphorylation without affecting the total amount of STAT5 protein. TG101209 inhibited Survivin and decreased STAT3 phosphorylation in HCC2429 and H460 lung cancer cells in vitro. TG101209 causes radiosensitization of HCC2429 and H460 lung cancer cells in vitro. A recent study showed that TG101209 abolished BCR-JAK2 and STAT5 phosphorylation, reduced expression by Bcl-xL, and caused apoptosis in transformed Ba/F3 cells. |
| In vivo study | 100 mg/kg of TG101209 effective prospects the survival in JAK2V617F-induced disease (10 days). Compared with placed EBO-treated animals, TG101209-treated animals observed statistically significant, dose-dependent reduction in the circulation tumor cell burden day +11 to 20%. 100 mg/kg TG101209 was effective in prolonging the survival time of JAK2V617F-induced diseased (10 days) animals. TG101209 treated animals exhibited a statistically significant, dose-dependent reduction in circulating tumor cell burden compared to placebo treated animals, reaching a 20% reduction at +11 days. |
CS-94 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.962 ml | 9.81 ml | 19.621 ml |
| 5 mM | 0.392 ml | 1.962 ml | 3.924 ml |
| 10 mM | 0.196 ml | 0.981 ml | 1.962 ml |
| 5 mM | 0.039 ml | 0.196 ml | 0.392 ml |
Last Update：2024-01-02 23:10:35
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CAS: 936091-14-4
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CAS: 936091-14-4
Tel: 18301782025
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Product Name: TG101209 Visit Supplier Webpage Request for quotation
CAS: 936091-14-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 936091-14-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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