research use only
Cat.No.S1176
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In vitro |
DMSO
: 67 mg/mL
(199.17 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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| Molecular Weight | 336.39 | Formula | C19H20N4O2 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 714272-27-2 | Download SDF | Storage of Stock Solutions |
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| Synonyms | NPI-2358 | SMILES | CC(C)(C)C1=C(N=CN1)C=C2C(=O)NC(=CC3=CC=CC=C3)C(=O)N2 | ||
Read more about storage stability stock solution CAS number SMILES
| Features |
Synthetic analog of NPI-2350 and greater potentcy than NPI-2350.
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|---|---|
| Targets/IC50/Ki |
Tubulin
9.8 nM-18 nM
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| In vitro |
NPI-2358 binds to the tubulin and has potent inhibitory to human tumor cell lines which have overexpressed Pgp or reduced nuclear Topo II catalytic activity, with IC50 from 9.8 to 18 nM. NPI-2358 is able to rapidly induce tubulin depolymerization in HUVECs and monolayer permeability even at 20 nM. NPI-2358 induces cell death in MM cells with IC50 of 8-10 nM, which due to trigger early mitotic arrest in MM cells. NPI-2358 also inhibits tubule formation and migration of endothelial as well as MM cells, which leads to disrupt tumor vasculature. NPI-2358 could induces cell death in patient MM (CD138+) cells without effecting viability of normal mononuclear cells. Blockade of JNK abrogates NPI-2358-induced mitotic arrest or MM cell death. |
| In vivo |
NPI-2358 (7.5 mg/kg) inhibits tumor growth in human plasmacytoma mouse xenograft models at well-tolerated doses. NPI-2358 induces a time- and dose-dependent decrease in tumour perfusion. NPI-2358 is more sensitive to the KHT sarcoma than the C3H tumour, while radiation response could enhance the antitumor activity in both models. |
References |
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(data from https://clinicaltrials.gov, updated on 2026-01-23)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT07361484 | NOT_YET_RECRUITING | Non-Small Cell Lung Cancer; Non-squamous Non-Small Cell Lung Cance |
BeyondSpring Pharmaceuticals Inc. |
2026-06-01 | PHASE3 |
| NCT05130827 | ACTIVE_NOT_RECRUITING | Multiple Myeloma |
Memorial Sloan Kettering Cancer Center |
2021-12-21 | PHASE2 |
| NCT05745350 | RECRUITING | Small Cell Lung Cancer Extensive Stage |
Xiaorong Dong |
2024-03-07 | PHASE2 |
| NCT05599789 | ACTIVE_NOT_RECRUITING | Non Small Cell Lung Cancer Metastatic |
Peking Union Medical College Hospital |
2023-02-01 | PHASE2 |
| NCT04902040 | TERMINATED | Advanced Bladder Carcinoma; Advanced Lung Non-Small Cell Carcinoma; Advanced Malignant Solid Neoplasm; Advanced Melanoma; Advanced Merkel Cell Carcinoma; Advanced Renal Cell Carcinoma; Clinical Stage III Cutaneous Melanoma AJCC v8; Clinical Stage III Merkel Cell Carcinoma AJCC v8; Clinical Stage IV Cutaneous Melanoma AJCC v8; Clinical Stage IV Merkel Cell Carcinoma AJCC v8; Pathologic Stage III Cutaneous Melanoma AJCC v8; Pathologic Stage III Merkel Cell Carcinoma AJCC v8; Pathologic Stage IIIA Cutaneous Melanoma AJCC v8; Pathologic Stage IIIA Merkel Cell Carcinoma AJCC v8; Pathologic Stage IIIB Cutaneous Melanoma AJCC v8; Pathologic Stage IIIB Merkel Cell Carcinoma AJCC v8; Pathologic Stage IIIC Cutaneous Melanoma AJCC v8; Pathologic Stage IIID Cutaneous Melanoma AJCC v8; Pathologic Stage IV Cutaneous Melanoma AJCC v8; Pathologic Stage IV Merkel Cell Carcinoma AJCC v8; Stage III Bladder Cancer AJCC v8; Stage III Lung Cancer AJCC v8; Stage III Renal Cell Cancer AJCC v8; Stage IIIA Bladder Cancer AJCC v8; Stage IIIA Lung Cancer AJCC v8; Stage IIIB Bladder Cancer AJCC v8; Stage IIIB Lung Cancer AJCC v8; Stage IIIC Lung Cancer AJCC v8; Stage IV Bladder Cancer AJCC v8; Stage IV Lung Cancer AJCC v8; Stage IV Renal Cell Cancer AJCC v8; Stage IVA Bladder Cancer AJCC v8; Stage IVA Lung Cancer AJCC v8; Stage IVB Bladder Cancer AJCC v8; Stage IVB Lung Cancer AJCC v8 |
M.D. Anderson Cancer Center |
2021-04-14 | PHASE1; PHASE2 |
| NCT02812667 | COMPLETED | Non-small Cell Lung Cancer Metastatic |
Lyudmila Bazhenova, M.D. |
2016-08-29 | PHASE1 |
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