| Size | Price | |
|---|---|---|
| 100mg | ||
| 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].
|
|---|---|
| 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 |
|
| Additional Infomation |
Tuspetinib (HM-43239) is under investigation in clinical trial NCT03850574 (Clinical Trial to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of HM43239 in Patients With Relapsed or Refractory Acute Myeloid Leukemia).
Tuspetinib is a selective, reversible type I inhibitor of FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2) with potential antineoplastic activity. Upon administration, tuspetinib reversibly binds to and inhibits the activity of FLT3. This inhibits the proliferation of FLT3-expressing cancer cells. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute myeloid leukemias. |
| Molecular Formula |
C29H33CLN6
|
|---|---|
| Molecular Weight |
501.0655
|
| Exact Mass |
500.245
|
| CAS # |
2294874-49-8
|
| PubChem CID |
135390910
|
| Appearance |
White to off-white solid powder
|
| LogP |
5.8
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
36
|
| Complexity |
725
|
| Defined Atom Stereocenter Count |
2
|
| 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]
|
| InChi Key |
FZLSDZZNPXXBBB-KDURUIRLSA-N
|
| InChi Code |
InChI=1S/C29H33ClN6/c1-17-4-7-24-25(12-31-27(24)8-17)28-26(30)13-32-29(35-28)34-23-10-20(9-22(11-23)21-5-6-21)16-36-14-18(2)33-19(3)15-36/h4,7-13,18-19,21,31,33H,5-6,14-16H2,1-3H3,(H,32,34,35)/t18-,19+
|
| Chemical Name |
5-chloro-N-[3-cyclopropyl-5-[[(3S,5R)-3,5-dimethylpiperazin-1-yl]methyl]phenyl]-4-(6-methyl-1H-indol-3-yl)pyrimidin-2-amine
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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)
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
