| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
Acute myeloid leukemia cell lines with FLT3 ITD mutations, such as MV4-11 (IC50: 1.3 nM), MOLM-13 (IC50: 5.1 nM), and MOLM-14 (IC50: 2.9 nM), are potently inhibited by tuspetinib in their proliferation. Tuspetinib causes the carbohydrate stem cell (LSC) marker KG1a cells to enlarge, and caspase 3/7 prevents KG1a cells (CD34+/CD38- cells) from proliferating [1]. In KG1a cells, tuspetinib can efficiently prevent SYK, STAT3, and STAT5 phosphorylation [3].
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|---|---|
| ln Vivo |
Tuspetinib showed good dose-proportional anti-tumor efficacy in mice models xenografted with MV4-11 and MOLM-13 cell lines without any major toxicity [1]. Tuspetinib can prolong the survival of FLT3 ITD/TKD double mutant xenograft mice [3].
|
| References |
[1]. Miyoung Lee, et.al. Abstract 804: Antitumor activity of the potent and novel FLT3 inhibitor HM43239 in acute myeloid leukemia. Cancer Res July 1 2018 (78) (13 Supplement) 804.
[2]. Naval G. Daver, et.al. HM43239, a Novel Potent Small Molecule FLT3 Inhibitor, in Acute Myeloid Leukemia (AML) with FMS-like Tyrosine Kinase 3 (FLT3) Mutations: Phase 1 /2 Study. Blood 2019; 134 (Supplement_1): 1331. [3]. JiSook Kim, et.al. Abstract 1293: HM43239, a novel FLT3 inhibitor in overcoming resistance for acute myeloid leukemia. Cancer Res July 1 2019 (79) (13 Supplement) 1293. |
| Molecular Formula |
C29H33CLN6
|
|---|---|
| Molecular Weight |
501.07
|
| CAS # |
2294874-49-8
|
| SMILES |
ClC1=C([H])N=C(N=C1C1=C([H])N([H])C2C([H])=C(C([H])([H])[H])C([H])=C([H])C1=2)N([H])C1=C([H])C(C([H])([H])N2C([H])([H])[C@@]([H])(C([H])([H])[H])N([H])[C@@]([H])(C([H])([H])[H])C2([H])[H])=C([H])C(=C1[H])C1([H])C([H])([H])C1([H])[H]
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~249.47 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9957 mL | 9.9786 mL | 19.9573 mL | |
| 5 mM | 0.3991 mL | 1.9957 mL | 3.9915 mL | |
| 10 mM | 0.1996 mL | 0.9979 mL | 1.9957 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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