| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 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].
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|---|---|
| ln Vivo |
KPT-8602 (15 mg/kg; daily dose; cavity feeding; 12 days) shows strong antioxidant bleaching activity [1].
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| 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 triazole compound with the structure 1H-1,2,4-triazole, substituted at positions 1 and 3 by (1E)-3-amino-3-oxo-2-(pyrimidin-5-yl)prop-1-en-1-yl and 3,5-bis(trifluoromethyl)phenyl, respectively. It is a second-generation export protein 1 inhibitor currently undergoing a phase II clinical trial for the treatment of patients with relapsed/refractory myelodysplastic syndromes. It exhibits a triple action of inhibiting export protein 1, antitumor activity, and inducing apoptosis. It belongs to the (trifluoromethyl)benzene, triazole, pyrimidine, enamide, and primary carboxamide classes. Eltanexor is being investigated in the clinical trial NCT02649790 (KPT-8602: Safety, Tolerability, and Efficacy Study in Patients with Relapsed/Refractory Cancer). Eltanexor is an orally bioavailable export protein-1 (XPO1; a homolog of chromosomal region maintenance protein 1; CRM1) inhibitor with potential antitumor activity. Upon administration, eltanexor binds to the cargo binding site of XPO1, thereby preventing XPO1-mediated nuclear export of cargo proteins (such as tumor suppressor proteins (TSPs), including p53, p73, BRCA1/2, pRB, FOXO, and other growth regulators), leading to the selective accumulation of these cargo proteins within the tumor cell nucleus. As a selective nuclear export inhibitor (SINE), KPT-8602 restores the nuclear localization and function of tumor suppressor proteins, thereby inducing tumor cell apoptosis. XPO1 is a major protein export factor responsible for transporting proteins from the nucleus to the cytoplasm. XPO1 is overexpressed in a variety of cancer cells, but expressed at extremely low levels in normal healthy cells. The export of tumor suppressor proteins to the cytoplasm prevents them from initiating apoptosis, leading to uncontrolled proliferation of tumor cells.
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| Molecular Formula |
C17H10F6N6O
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|---|---|
| Molecular Weight |
428.2984
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| Exact Mass |
428.082
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| CAS # |
1642300-52-4
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| Related CAS # |
Eltanexor Z-isomer;1642300-78-4
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| PubChem CID |
86345880
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
574.4±60.0 °C at 760 mmHg
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| Flash Point |
301.2±32.9 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.594
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| LogP |
2.83
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
626
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| Defined Atom Stereocenter Count |
0
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| 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
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| InChi Key |
JFBAVWVBLRIWHM-AWNIVKPZSA-N
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| 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+
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| Chemical Name |
(E)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-2-pyrimidin-5-ylprop-2-enamide
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| Synonyms |
KPT-8602 KPT8602 KPT 8602. Eltanexor.
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~233.49 mM)
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| 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.
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