| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| References |
|
|---|---|
| Additional Infomation |
Enzastaurin Hydrochloride is the hydrochloride salt of enzastaurin, a synthetic macrocyclic bisindomaleimide with potential antitumor activity. Enzastaurin binds to ATP-binding sites and selectively inhibits protein kinase Cβ, an enzyme involved in inducing vascular endothelial growth factor (VEGF)-stimulated angiogenesis. This drug may reduce the blood supply to tumors, thereby alleviating the tumor burden. See also: Enzastaurin (with active fraction).
|
| Molecular Formula |
C32H30CLN5O2
|
|---|---|
| Molecular Weight |
552.07
|
| Exact Mass |
551.209
|
| CAS # |
359017-79-1
|
| PubChem CID |
176166
|
| Appearance |
Typically exists as solids at room temperature
|
| Boiling Point |
767.2ºC at 760 mmHg
|
| Flash Point |
417.8ºC
|
| LogP |
6.001
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
40
|
| Complexity |
974
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
Cl.C1=CC=C(CN2CCC(N3C=C(C4C(=O)NC(=O)C=4C4=CN(C)C5=CC=CC=C45)C4=CC=CC=C34)CC2)N=C1
|
| InChi Key |
UUADYKVKJIMIPA-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C32H29N5O2.ClH/c1-35-19-25(23-9-2-4-11-27(23)35)29-30(32(39)34-31(29)38)26-20-37(28-12-5-3-10-24(26)28)22-13-16-36(17-14-22)18-21-8-6-7-15-33-21;/h2-12,15,19-20,22H,13-14,16-18H2,1H3,(H,34,38,39);1H
|
| Chemical Name |
3-(1-methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrrole-2,5-dione;hydrochloride
|
| Synonyms |
LY317615 hydrochloride
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8114 mL | 9.0568 mL | 18.1136 mL | |
| 5 mM | 0.3623 mL | 1.8114 mL | 3.6227 mL | |
| 10 mM | 0.1811 mL | 0.9057 mL | 1.8114 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.
Link: https://clinicaltrials.gov/ct2/show/NCT03263026
Conditions:Diffuse Large B-Cell LymphomaLink: https://clinicaltrials.gov/ct2/show/NCT03776071
Conditions:GlioblastomaLink: https://clinicaltrials.gov/ct2/show/NCT00192114
Conditions:Colonic Neoplasms
Title:LY317615 Plus Capecitabine in Treating Patients With Advanced Solid Tumors
Status:Completed
updateDate:2020-08-03
Ctid:NCT00052273
Link: https://clinicaltrials.gov/ct2/show/NCT00052273
Conditions:Adult|Solid TumorLink: https://clinicaltrials.gov/ct2/show/NCT00407758
Conditions:Ovarian Cancer|Primary Peritoneal Cavity CancerLink: https://clinicaltrials.gov/ct2/show/NCT00469976
Conditions:Lung CancerLink: https://clinicaltrials.gov/ct2/show/NCT00516607
Conditions:Brain and Central Nervous System TumorsLink: https://clinicaltrials.gov/ct2/show/NCT00685633
Conditions:Prostate CancerLink: https://clinicaltrials.gov/ct2/show/NCT00550927
Conditions:Unspecified Adult Solid Tumor, Protocol SpecificLink: https://clinicaltrials.gov/ct2/show/NCT00503724
Conditions:Brain and Central Nervous System Tumors|NeuroblastomaLink: https://clinicaltrials.gov/ct2/show/NCT00386087
Conditions:Breast NeoplasmsLink: https://clinicaltrials.gov/ct2/show/NCT00105092
Conditions:Non-Small-Cell Lung CarcinomaLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2007-003844-31
Condition:Locally advanced or metastatic Colorectal CancerLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2006-005306-31
Condition:advanced, unresectable, or metastatic (stage IIIB or IV) non-small cell lung cancerLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2007-000281-21
Condition:primary glioma without methylation of the promoter gene of MGMT enzymeLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2006-006698-25
Condition:Advanced or Metastatic Non Small Cell Lung CancerLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2006-005305-58
Condition:metastatic breast cancer, resistant to aromatase inhibitorsLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2006-001985-17
Condition:high-risk diffuse large B-cell lymphoma (DLBCL )Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2006-004486-34
Condition:Have a histologic or cytologic diagnosis of advanced or metastatic malignancies for which no life-prolonging therapy exists and have been previously enrolled and completed therapy in an enzastaurin clinical pharmacology and biopharmaceutics study.Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2006-002316-10
Condition:Patients with a histologic diagnosis of FIGO Stage IIB, IIC, III, or IV advanced invasive epithelial ovarian, fallopian tube, or peritoneal carcinoma.Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2006-000889-36
Condition:brain metastastases of non-small or small cell lung cancerLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2005-004627-18
Condition:GlioblastomaLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2005-004630-41
Condition:High-risk Diffuse Large B-cell Lymphoma (DLBCL )Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2004-005068-26
Condition:metastatic colorectal cancerProducts are for research use only; We do not sell to patients
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