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Enzastaurin hydrochloride

别名: LY317615 hydrochloride
目录号: V93659
COA 产品数据 产品说明书 SDS
Enzastaurin (LY317615) 盐酸盐是一种有效的 PKCβ 抑制剂，IC50 值为 6 nM。
Enzastaurin hydrochloride CAS号: 359017-79-1
产品类别: Apoptosis | 凋亡
产品仅用于科学研究，不针对患者销售
规格 价格
500mg
1g
Other Sizes
大包装询价
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InvivoChem产品被CNS等顶刊论文引用
产品描述
Enzastaurin (LY317615) 盐酸盐是一种有效的 PKCβ 抑制剂，IC50 值为 6 nM。Enzastaurin 盐酸盐对 PKCβ 的选择性比对 PKCα、PKCγ 和 PKCε 的选择性高 6-20 倍。
生物活性&实验参考方法
参考文献

[1]. The protein kinase Cbeta-selective inhibitor, Enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts. Cancer Res, 2005, 65(16),

[2]. Inhibition of glycogen synthase kinase-3 increases the cytotoxicity of enzastaurin. J Invest Dermatol, 2011, 131(7), 1442-1449.

[3]. Targeting PKC in multiple myeloma: in vitro and in vivo effects of the novel, orally available small-molecule inhibitor enzastaurin (LY317615.HCl). Blood, 2007, 109(4), 1669-1677.
其他信息
盐酸恩扎司他林是恩扎司他林的盐酸盐，恩扎司他林是一种合成的大环双吲哚马来酰亚胺，具有潜在的抗肿瘤活性。恩扎司他林与ATP结合位点结合，选择性抑制蛋白激酶Cβ，该酶参与诱导血管内皮生长因子（VEGF）刺激的新血管生成。该药物可能减少肿瘤的血液供应，从而减轻肿瘤负荷。
另见：恩扎司他林（具有活性部分）。
*注: 文献方法仅供参考, InvivoChem并未独立验证这些方法的准确性
化学信息 & 存储运输条件
分子式
C32H30CLN5O2
分子量
552.07
精确质量
551.209
CAS号
359017-79-1
PubChem CID
176166
外观&性状
Typically exists as solids at room temperature
沸点
767.2ºC at 760 mmHg
闪点
417.8ºC
LogP
6.001
tPSA
72.16
氢键供体(HBD)数目
2
氢键受体(HBA)数目
4
可旋转键数目(RBC)
5
重原子数目
40
分子复杂度/Complexity
974
定义原子立体中心数目
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
化学名
3-(1-methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrrole-2,5-dione;hydrochloride
别名
LY317615 hydrochloride
HS Tariff Code
2934.99.9001
存储方式

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month
运输条件
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
溶解度数据
溶解度 (体外实验)
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
溶解度 (体内实验)
注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。
注射用配方
(IP/IV/IM/SC等)
注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。
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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

口服配方
口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。
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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。
请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。
制备储备液 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

1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;

2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;

3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;

4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。

计算器
计算 重置

摩尔浓度计算器可计算特定溶液所需的质量、体积/浓度，具体如下：

  • 计算制备已知体积和浓度的溶液所需的化合物的质量
  • 计算将已知质量的化合物溶解到所需浓度所需的溶液体积
  • 计算特定体积中已知质量的化合物产生的溶液的浓度
使用摩尔浓度计算器计算摩尔浓度的示例如下所示：
假如化合物的分子量为350.26 g/mol，在5mL DMSO中制备10mM储备液所需的化合物的质量是多少？
  • 在分子量（MW）框中输入350.26
  • 在“浓度”框中输入10，然后选择正确的单位（mM）
  • 在“体积”框中输入5，然后选择正确的单位（mL）
  • 单击“计算”按钮
  • 答案17.513 mg出现在“质量”框中。以类似的方式，您可以计算体积和浓度。
计算 重置

稀释计算器可计算如何稀释已知浓度的储备液。例如，可以输入C1、C2和V2来计算V1，具体如下：

制备25毫升25μM溶液需要多少体积的10 mM储备溶液？
使用方程式C1V1=C2V2，其中C1=10mM，C2=25μM，V2=25 ml，V1未知：
  • 在C1框中输入10，然后选择正确的单位（mM）
  • 在C2框中输入25，然后选择正确的单位（μM）
  • 在V2框中输入25，然后选择正确的单位（mL）
  • 单击“计算”按钮
  • 答案62.5μL（0.1 ml）出现在V1框中
g/mol
计算 重置

分子量计算器可计算化合物的分子量 (摩尔质量)和元素组成，具体如下：

注：化学分子式大小写敏感：C12H18N3O4  c12h18n3o4
计算化合物摩尔质量（分子量）的说明：
  • 要计算化合物的分子量 (摩尔质量)，请输入化学/分子式，然后单击“计算”按钮。
分子质量、分子量、摩尔质量和摩尔量的定义：
  • 分子质量（或分子量）是一种物质的一个分子的质量，用统一的原子质量单位（u）表示。（1u等于碳-12中一个原子质量的1/12）
  • 摩尔质量（摩尔重量）是一摩尔物质的质量，以g/mol表示。
/
计算 重置

配液计算器可计算将特定质量的产品配成特定浓度所需的溶剂体积 (配液体积)

  • 输入试剂的质量、所需的配液浓度以及正确的单位
  • 单击“计算”按钮
  • 答案显示在体积框中
动物体内实验配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶/难溶于水的化合物），不同的产品和批次配方组成不同，如对配方有疑问，可先联系我们提供正确的体内实验配方。此外，请注意这只是一个配方计算器，而不是特定产品的确切配方。
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+
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计算 重置

计算结果:

工作液浓度： mg/mL；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。

(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
            (2) 一定要按顺序加入溶剂 (助溶剂) 。

临床试验信息
Title:Study to Assess Enzastaurin + R-CHOP in Subjects With DLBCL With the Genomic Biomarker DGM1™
Status:Completed
updateDate:2025-01-23
Ctid:NCT03263026

Link: https://clinicaltrials.gov/ct2/show/NCT03263026

Conditions:Diffuse Large B-Cell Lymphoma
Interventions:Enzastaurin Hydrochloride
Phase:Phase 3
Title:A Trial of Enzastaurin Plus Temozolomide During and Following Radiation Therapy in Patients With Newly Diagnosed Glioblastoma With or Without the Novel Genomic Biomarker, DGM1
Status:Completed
updateDate:2024-04-22
Ctid:NCT03776071

Link: https://clinicaltrials.gov/ct2/show/NCT03776071

Conditions:Glioblastoma
Interventions:Temozolomide
Phase:Phase 3
Title:Enzastaurin for Patients With Metastatic Colorectal Cancer
Status:Completed
updateDate:2020-08-06
Ctid:NCT00192114

Link: https://clinicaltrials.gov/ct2/show/NCT00192114

Conditions:Colonic Neoplasms
Interventions:Enzastaurin HCl
Phase:Phase 2
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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 Tumor
Interventions:enzastaurin hydrochloride
Phase:Phase 1
Title:Enzastaurin in Treating Patients With Persistent or Recurrent Ovarian Epithelial Cancer or Primary Peritoneal Cancer
Status:Completed
updateDate:2019-03-20
Ctid:NCT00407758

Link: https://clinicaltrials.gov/ct2/show/NCT00407758

Conditions:Ovarian Cancer|Primary Peritoneal Cavity Cancer
Interventions:enzastaurin hydrochloride
Phase:Phase 2
Title:Enzastaurin, Carboplatin, and Gemcitabine With or Without Bevacizumab in Treating Patients With Recurrent, Stage IIIB, or Stage IV Non-Small Cell Lung Cancer
Status:Withdrawn
updateDate:2015-10-08
Ctid:NCT00469976

Link: https://clinicaltrials.gov/ct2/show/NCT00469976

Conditions:Lung Cancer
Interventions:gemcitabine hydrochloride
Phase:Phase 2
Title:Enzastaurin and Temozolomide in Treating Patients With Primary Gliomas
Status:Unknown status
updateDate:2015-02-10
Ctid:NCT00516607

Link: https://clinicaltrials.gov/ct2/show/NCT00516607

Conditions:Brain and Central Nervous System Tumors
Interventions:temozolomide
Phase:Phase 1
Title:Bicalutamide With or Without Enzastaurin in Treating Patients With Prostate Cancer
Status:Withdrawn
updateDate:2013-08-20
Ctid:NCT00685633

Link: https://clinicaltrials.gov/ct2/show/NCT00685633

Conditions:Prostate Cancer
Interventions:enzastaurin hydrochloride
Phase:Phase 2
Title:Enzastaurin and Bevacizumab in Treating Patients With Locally Advanced or Metastatic Cancer
Status:Completed
updateDate:2013-05-15
Ctid:NCT00550927

Link: https://clinicaltrials.gov/ct2/show/NCT00550927

Conditions:Unspecified Adult Solid Tumor, Protocol Specific
Interventions:enzastaurin hydrochloride
Phase:Phase 1
Title:Enzastaurin in Treating Young Patients With Refractory Primary CNS Tumors
Status:Completed
updateDate:2012-03-06
Ctid:NCT00503724

Link: https://clinicaltrials.gov/ct2/show/NCT00503724

Conditions:Brain and Central Nervous System Tumors|Neuroblastoma
Interventions:enzastaurin hydrochloride
Phase:Phase 1
Title:Enzastaurin For Breast Cancer Patients Who Previously Received an Anthracycline and a Taxane Chemotherapy
Status:Completed
updateDate:2008-06-06
Ctid:NCT00386087

Link: https://clinicaltrials.gov/ct2/show/NCT00386087

Conditions:Breast Neoplasms
Interventions:Enzastaurin Hydrochloride
Phase:Phase 2
Title:Enzastaurin as Second and Third-Line Treatment for Non-Small Cell Lung Cancer.
Status:Completed
updateDate:2007-05-01
Ctid:NCT00105092

Link: https://clinicaltrials.gov/ct2/show/NCT00105092

Conditions:Non-Small-Cell Lung Carcinoma
Interventions:Enzastaurin HCL
Phase:Phase 2
Title:A Double-Blind, Randomized, Placebo-Controlled, Phase 2 Study of Enzastaurin with 5 FU/LV plus Bevacizumab as Maintenance Regimen Following First Line Therapy for Metastatic Colorectal Cancer
Status:Completed, Prematurely Ended
Date:2007-11-28
Eudractnumber:2007-003844-31

Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2007-003844-31

Condition:Locally advanced or metastatic Colorectal Cancer
Phase:Phase 2
Title:Randomized, Double-Blind, Placebo-Controlled, Phase 2 Study of Pemetrexed and Cisplatin plus Enzastaurin versus Pemetrexed and Cisplatin plus Placebo in Chemonaive Patients with Advanced, Unresectable, or Metastatic (Stage IIIB or IV) Non-Small Cell Lung Cancer
Status:Completed, Prematurely Ended
Date:2007-09-20
Eudractnumber:2006-005306-31

Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2006-005306-31

Condition:advanced, unresectable, or metastatic (stage IIIB or IV) non-small cell lung cancer
Phase:Phase 2
Title:Enzastaurin (LY317615) Before and Concomitant with Radiation Therapy, Followed by Enzastaurin Maintenance Therapy in Patients with Newly Diagnosed Glioblastoma without Methylation of the Promoter Gene of MGMT Enzyme
Status:Completed
Date:2007-09-05
Eudractnumber:2007-000281-21

Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2007-000281-21

Condition:primary glioma without methylation of the promoter gene of MGMT enzyme
Phase:Phase 2
Title:A Phase 2 Double-Blind Randomized Study of Oral Enzastaurin HCl versus Placebo Concurrently with Pemetrexed (Alimta®) as Second Line Therapy in Patients with Advanced or Metastatic Non Small Cell Lung Cancer
Status:Completed, Prematurely Ended
Date:2007-07-23
Eudractnumber:2006-006698-25

Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2006-006698-25

Condition:Advanced or Metastatic Non Small Cell Lung Cancer
Phase:Phase 2
Title:A Randomized, Double-Blind, Phase 2 Trial of Fulvestrant Plus Enzastaurin versus Fulvestrant Plus Placebo in Aromatase Inhibitor-Resistant Metastatic Breast Cancer
Status:Completed
Date:2007-04-12
Eudractnumber:2006-005305-58

Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2006-005305-58

Condition:metastatic breast cancer, resistant to aromatase inhibitors
Phase:Phase 2
Title:An Open-label, Single Arm, Phase 2 Study of Rituximab, Gemcitabine, and Oxaliplatin plus Oral Enzastaurin as Treatment for Patients with
Status:Completed
Date:2006-10-25
Eudractnumber:2006-001985-17

Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2006-001985-17

Condition:high-risk diffuse large B-cell lymphoma (DLBCL )
Phase:Phase 2
Title:An Open-Label Study of Oral Enzastaurin HCI in Patients with Advanced or Metastatic Malignancies
Status:Completed
Date:2006-10-18
Eudractnumber:2006-004486-34

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.
Phase:Phase 2
Title:A Randomized, Phase 2, Placebo-Controlled, Double-Blinded Study With and Without Enzastaurin in Combination With Paclitaxel and Carboplatin as First-Line Treatment, Followed by Maintenance Treatment in Advanced Ovarian Cancer
Status:Completed
Date:2006-10-09
Eudractnumber:2006-002316-10

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.
Phase:Phase 2
Title:A Double-blind, Randomized, Placebo-controlled Multicentre Phase II Study of Maintenance Enzastaurin Following Whole Brain Radiation Therapy in the Treatment of Brain Metastases from Lung Cancer
Status:Completed, Prematurely Ended
Date:2006-08-10
Eudractnumber:2006-000889-36

Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2006-000889-36

Condition:brain metastastases of non-small or small cell lung cancer
Phase:Phase 2
Title:A Randomized Phase 3 Study of Enzastaurin versus Lomustine in the Treatment of Recurrent, Intracranial Glioblastoma Multiforme
Status:Completed, Prematurely Ended
Date:2006-08-04
Eudractnumber:2005-004627-18

Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2005-004627-18

Condition:Glioblastoma
Phase:Phase 3
Title:A Phase 3 Clinical Study to Investigate the Prevention of Relapse in Lymphoma Using Daily Enzastaurin
Status:Completed, Prematurely Ended
Date:2006-04-26
Eudractnumber:2005-004630-41

Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2005-004630-41

Condition:High-risk Diffuse Large B-cell Lymphoma (DLBCL )
Phase:Phase 3
Title:A Phase 2 Study of Oral Enzastaurin HCl in Patients with Metastatic Colorectal Cancer
Status:Completed
Date:2005-06-17
Eudractnumber:2004-005068-26

Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2004-005068-26

Condition:metastatic colorectal cancer
Phase:Phase 2

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