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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Ispinesib (formerly also known as CK-0238273, SB-715992), a quinazolinone analog, is a novel, specific and reversible inhibitor of kinesin spindle protein (KSP, a mitotic motor protein) with potential antineoplastic activity. It inhibits KSP with a Ki app of 1.7 nM in a cell-free assay, and exhibits no effects on closely related target proteins such as CENP-E, RabK6, MCAK, MKLP1, KHC or Kif1A. Ispinesib is derived from quinazolinone with anticancer properties. It acts by selectively inhibiting the mitotic motor protein, kinesin spindle protein (KSP), resulting in inhibition of mitotic spindle assembly, induction of cell cycle arrest, and cell death.
| ln Vitro |
Having a Ki app of 1.7 nM, ispinesib is a strong and very selective inhibitor of KSP[1]. BT-474 and MDA-MB-468 cell lines are inhibited by ispinesib (150 nM), with GI50s of 45 and 19 nM, respectively[2]. Ispinesib (SB715992, 15 and 30 nM) causes prostate cancer cells to undergo apoptosis by 1094.88% and 1516.70%, respectively, and suppresses PC-3 prostate cancer cell proliferation by 48.65% and 52.16%. Genes involved in cell cycle arrest and apoptosis are upregulated by ispinenesib, whereas genes involved in cell survival and proliferation are downregulated. Genistein can augment ispinenesib's pro-apoptotic and anti-proliferation properties[3].
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| ln Vivo |
In mice containing tumor xenografts of ER-positive (MCF7), HER2-positive (KPL4, HCC1954, and BT-474), and triple-negative (MDA-MB-468) breast cancer cells, iminetsinib (SCID, 8 mg/kg; nude, 10 mg/kg, q4d × 3) decreases tumor volume by an intraperitoneal injection given three times[2].
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| Additional Infomation |
N-(3-aminopropyl)-N-[(1R)-1-[7-chloro-4-oxo-3-(phenylmethyl)-2-quinazolinyl]-2-methylpropyl]-4-methylbenzamide is a member of benzamides.
Ispinesib is a synthetic small molecule, derived from quinazolinone, with antineoplastic properties. Ispinesib selectively inhibits the mitotic motor protein, kinesin spindle protein (KSP), resulting in inhibition of mitotic spindle assembly, induction of cell cycle arrest during the mitotic phase, and cell death in tumor cells that are actively dividing. Because KSP is not involved in nonmitotic processes, such as neuronal transport, ispinesib may be less likely to cause the peripheral neuropathy often associated with the tubulin-targeting agents. Drug Indication Investigated for use/treatment in breast cancer, lung cancer, solid tumors, renal cell carcinoma, pediatric indications, ovarian cancer, and head and neck cancer. |
| Molecular Formula |
C30H33CLN4O2
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|---|---|---|
| Molecular Weight |
517.06
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| Exact Mass |
516.229
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| CAS # |
336113-53-2
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| Related CAS # |
336113-53-2;514820-03-2 (mesylate);
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| PubChem CID |
6851740
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| Appearance |
White to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
708.0±70.0 °C at 760 mmHg
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| Flash Point |
382.0±35.7 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.619
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| LogP |
5.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
37
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| Complexity |
803
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1=CC=C(C=C1)C(=O)N(CCCN)[C@@H](C2=NC3=C(C=CC(=C3)Cl)C(=O)N2CC4=CC=CC=C4)C(C)C
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| InChi Key |
QJZRFPJCWMNVAV-HHHXNRCGSA-N
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| InChi Code |
InChI=1S/C30H33ClN4O2/c1-20(2)27(34(17-7-16-32)29(36)23-12-10-21(3)11-13-23)28-33-26-18-24(31)14-15-25(26)30(37)35(28)19-22-8-5-4-6-9-22/h4-6,8-15,18,20,27H,7,16-17,19,32H2,1-3H3/t27-/m1/s1
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| Chemical Name |
(R)-N-(3-aminopropyl)-N-(1-(3-benzyl-7-chloro-4-oxo-3,4-dihydroquinazolin-2-yl)-2-methylpropyl)-4-methylbenzamide
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| Synonyms |
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.84 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 (4.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 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 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 | 1.9340 mL | 9.6701 mL | 19.3401 mL | |
| 5 mM | 0.3868 mL | 1.9340 mL | 3.8680 mL | |
| 10 mM | 0.1934 mL | 0.9670 mL | 1.9340 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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