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Selinexor (KPT-330)
🥰Excellent
Catalog No. T6106Cas No. 1393477-72-9
Alias Selinexor, KPT-330
Selinexor (KPT-330) is a small molecule inhibitor of CRM1 with selective and oral activity. Selinexor blocks the cell cycle, induces apoptosis, and has antitumor activity for the treatment of multiple myeloma.
Selinexor (KPT-330)
🥰Excellent
Purity: 100%
Catalog No. T6106Alias Selinexor, KPT-330Cas No. 1393477-72-9
Selinexor (KPT-330) is a small molecule inhibitor of CRM1 with selective and oral activity. Selinexor blocks the cell cycle, induces apoptosis, and has antitumor activity for the treatment of multiple myeloma.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $39 | In Stock | |
| 5 mg | $74 | In Stock | |
| 25 mg | $281 | In Stock | |
| 50 mg | $422 | In Stock | |
| 100 mg | $481 | In Stock |
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(E)-KPT330
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CRM1-IN-1 (Compound KL1), a noncovalent inhibitor of CRM1, promotes nuclear degradation of CRM1 with an IC50 of 0.27 μM, inhibits CRM1-mediated nuclear export, suppresses cell proliferation, and induces apoptosis in colorectal cancer cells [1].
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CRM1-IN-2
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CRM1-IN-2 (Compound KL2) is a noncovalent inhibitor of CRM1, localizing it to the nuclear periphery, reducing its nuclear presence, and inhibiting its nuclear export function. It effectively inhibits the growth of colorectal cancer cells and induces apoptosis [1].
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Leptomycin B
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Leptomycin B (LMB) is a potent inhibitor of the nuclear export of proteins and is a potent antifungal antibiotic blocking the eukaryotic cell cycle. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue.
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Leptomycin A
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Leptomycin A, a metabolite derived from Streptomyces, acts as an inhibitor of CRM1 (exportin 1) and effectively suppresses HIV-1 replication. Compared to Leptomycin B, it exhibits lesser potency. Leptomycin A hampers the interaction between CRM1 and nuclear export signals, effectively hindering the nuclear export of a wide array of proteins.
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CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activity.CBS9106 inhibits CRM1-dependent nuclear export and reduces CRM1 protein levels.CBS9106 inhibits tumor growth and prolongs the survival of mice bearing tumor xenografts.CBS9106 is an inhibitor of CRM1-dependent nuclear export and reduces CRM1 protein levels.
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Verdinexor Cited
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Verdinexor (KPT-335) (KPT-335), a specific XPO1/CRM1 inhibitor, are orally bioavailable.
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SP100030 analogue 1 (compound 11) is a selective transcription activation (SITA) inhibitor within the SP100030 class, capable of inhibiting XPO1-dependent upregulation of IL2 in a Jurkat-based IL2-Luc reporter assay, with an EC50 of 137 nM.
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Purity:100%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Selinexor (KPT-330) is a small molecule inhibitor of CRM1 with selective and oral activity. Selinexor blocks the cell cycle, induces apoptosis, and has antitumor activity for the treatment of multiple myeloma. |
| In vitro | METHODS: Six T-ALL cells, MOLT-4, Jurkat, HBP-ALL, KOPTK-1, SKW-3 and DND-41, were treated with Selinexor (0-1000 µM) for 72 h. Cell growth inhibition was detected using Cell Titer Glo assay. RESULTS: Selinexor treatment inhibited T-ALL cell growth with IC50 values of 34-203 nM. [1] METHODS: Multiple myeloma cells MM1S were treated with Selinexor (100 nM) for 8 h. The expression levels of target proteins were detected by Western Blot. RESULTS: Selinexor treatment resulted in the accumulation of p53, IκB, p21 and p27 in the nucleus of MM1S cells. [2] |
| In vivo | METHODS: To assay antitumor activity in vivo, Selinexor (20-25 mg/kg) was administered by gavage to NSG mice harboring the human T-ALL tumor MOLT-4 three times per week for thirty-six days. RESULTS: Selinexor-treated mice exhibited significant inhibition of leukemia cell growth with significant survival benefit. [1] METHODS: To assay anti-tumor activity in vivo, Selinexor (20 mg/kg) was administered by gavage three times per week for four weeks to an NSG mouse model of primary AML in patients. RESULTS: Selinexor was cytotoxic to primary AML cells transplanted into mice. [3] |
| Alias | Selinexor, KPT-330 |
| Molecular Weight | 443.31 |
| Formula | C17H11F6N7O |
| Cas No. | 1393477-72-9 |
| Smiles | FC(F)(F)c1cc(cc(c1)C(F)(F)F)-c1ncn(\C=C/C(=O)NNc2cnccn2)n1 |
| Relative Density. | 1.55 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 38 mg/mL (85.72 mM), Sonication is recommended. DMSO: 55 mg/mL (124.07 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 8.2 mg/mL (18.5 mM), In vivo: Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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