| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Eltanexor (is discontinued) formerly known as KPT-8602, is a second-generation exportin-1 inhibitor. KPT-8602 displays potent activity against acute lymphoblastic leukemia. KPT-8602 is well tolerated and highly active against AML blasts and leukemia-initiating cells. Eltanexor shows improved efficacy and in vivo tolerability in hematological malignancies.
| ln Vitro |
KPT-8602 (15 mg/kg; oral gavage; daily for 12 days) demonstrates strong anti-lymphoblastic leukemia efficacy[1].
|
|---|---|
| ln Vivo |
KPT-8602 (15 mg/kg; daily dose; cavity feeding; 12 days) shows strong antioxidant bleaching activity [1].
|
| Cell Assay |
Cell viability assay[1]
Cell Types: T-ALL cells (Jurkat, MOLT-4 , ALL-SIL, DND41 and HPB-ALL), B-ALL cells (BV173, EHEB and REH), AML cells (MV4-11, MOLM13, K-562 and HL-60) Tested Concentrations: 2, 4, 6 nM Incubation Duration: 72 hrs (hours) Experimental Results: diminished cell viability with EC50 values ranging from 25 to 145 nM. Western Blot Analysis[1] Cell Types: T-ALL, B-ALL, AML Cell Tested Concentrations: 1 μM Incubation Duration: 16 Experimental Results: Earliest 6 Cleaved caspase-3 substrate PARP appears within hrs (hours). |
| Animal Protocol |
Animal/Disease Models: Female balb/c (Bagg ALBino) mouse (model using JAK3 (M511I) mutation) [1]
Doses: 15 mg/kg Route of Administration: po (oral gavage); one time/day for 12 days Experimental Results: Comparable to placebo-treated animals After 2 days of treatment, the total white blood cell (WBC) count was Dramatically diminished, and the WBC count continued to decrease until reaching normal levels (<10,000 cells/μL) on day 12. |
| References | |
| Additional Infomation |
Eltanexor is a member of the class of triazoles that is 1H-1,2,4-triazole substituted by (1E)-3-amino-3-oxo-2-(pyrimidin-5-yl)prop-1-en-1-yl and 3,5-bis(trifluoromethyl)phenyl groups at positions 1 and 3, respectively. It is a second-generation exportin 1 inhibitor that is currently in phase II clinical trial for the treatment of patients with higher relapsed/refractory myelodysplastic neoplasms. It has a role as an exportin 1 inhibitor, an antineoplastic agent and an apoptosis inducer. It is a member of (trifluoromethyl)benzenes, a member of triazoles, a member of pyrimidines, an enamide and a primary carboxamide.
Eltanexor is under investigation in clinical trial NCT02649790 (Study of the Safety, Tolerability and Efficacy of KPT-8602 in Patients With Relapsed/refractory Cancer Indications). Eltanexor is an orally bioavailable inhibitor of exportin-1 (XPO1; chromosome region maintenance 1 protein homolog; CRM1), with potential antineoplastic activity. Upon administration, eltanexor binds to the XPO1 cargo binding site, which prevents the XPO1-mediated nuclear export of cargo proteins such as tumor suppressor proteins (TSPs), including p53, p73, BRCA1/2, pRB, FOXO, and other growth regulatory proteins and leads to their selective accumulation in the nuclei of tumor cells. As a selective inhibitor of nuclear export (SINE), KPT-8602 restores the nuclear localization and function of tumor suppressing proteins which leads to the induction of apoptosis in tumor cells. XPO1, the major export factor that transports proteins from the nucleus to the cytoplasm, is overexpressed in a variety of cancer cell types while minimally expressed in normal, healthy cells. The export of tumor suppressor proteins into the cytoplasm prevents them from initiating apoptosis and leads to uncontrolled tumor cell proliferation. |
| Molecular Formula |
C17H10F6N6O
|
|---|---|
| Molecular Weight |
428.2984
|
| Exact Mass |
428.082
|
| CAS # |
1642300-52-4
|
| Related CAS # |
Eltanexor Z-isomer;1642300-78-4
|
| PubChem CID |
86345880
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
1.6±0.1 g/cm3
|
| Boiling Point |
574.4±60.0 °C at 760 mmHg
|
| Flash Point |
301.2±32.9 °C
|
| Vapour Pressure |
0.0±1.6 mmHg at 25°C
|
| Index of Refraction |
1.594
|
| LogP |
2.83
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
30
|
| Complexity |
626
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=C(C=C(C=C1C(F)(F)F)C(F)(F)F)C2=NN(C=N2)/C=C(\C3=CN=CN=C3)/C(=O)N
|
| InChi Key |
JFBAVWVBLRIWHM-AWNIVKPZSA-N
|
| InChi Code |
InChI=1S/C17H10F6N6O/c18-16(19,20)11-1-9(2-12(3-11)17(21,22)23)15-27-8-29(28-15)6-13(14(24)30)10-4-25-7-26-5-10/h1-8H,(H2,24,30)/b13-6+
|
| Chemical Name |
(E)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-2-pyrimidin-5-ylprop-2-enamide
|
| Synonyms |
KPT-8602 KPT8602 KPT 8602. Eltanexor.
|
| 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 |
| 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 : ≥ 100 mg/mL (~233.49 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.84 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3348 mL | 11.6741 mL | 23.3481 mL | |
| 5 mM | 0.4670 mL | 2.3348 mL | 4.6696 mL | |
| 10 mM | 0.2335 mL | 1.1674 mL | 2.3348 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
COA