Home PI3K/Akt/mTOR PI3K inhibitor - Autophagy activator Idelalisib (CAL-101) 仅限科研使用

Idelalisib (CAL-101)

别名: GS-1101 中文名称：艾代拉里斯，艾代拉利司

Idelalisib (CAL-101)是选择性p110δ抑制剂，在无细胞试验中IC50为 2.5 nM；对 p110δ 表现出的选择性是对 p110α/β/γ 的 40 到 300 倍，对p110δ的选择性是对 C2β，hVPS34，DNA-PK 和 mTOR的400到4000倍。Idelalisib 还可诱导自噬。

Idelalisib (CAL-101) Chemical Structure

Idelalisib (CAL-101) Chemical Structure

CAS: 870281-82-6

规格 价格 库存 购买数量
10mM (1mL in DMSO) 737.1 现货
10mg 647.01 现货
50mg 1941.03 现货
200mg 4832.1 现货
1g 15315.3 现货
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Idelalisib (CAL-101)相关产品

相关信号通路图

PI3K Signaling Pathways

PI3K信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息(PMID)
SR786 Growth Inhibition Assay 10 μM 72 h does not induce apoptosis 22801959
Myla Growth Inhibition Assay 10 μM 72 h does not induce apoptosis 22801959
HH Growth Inhibition Assay 10 μM 72 h Induction of apoptosis slightly 22801959
SP53 Growth Inhibition Assay 0.1 μM 72 h does not induce cell cycle arrest or apoptosis 23676220
MINO Growth Inhibition Assay 5 μM 72 h does not induce cell cycle arrest or apoptosis 23676220
MAVER-1 Growth Inhibition Assay 5 μM 72 h does not induce cell cycle arrest or apoptosis 23676220
JEKO-1 Growth Inhibition Assay 5 μM 72 h does not induce cell cycle arrest or apoptosis 23676220
JEKO-1 Growth Inhibition Assay 10 μM 72 h Inhibition of proliferation slightly 23341541
Granta-519 Function Assay 1 μM 2 h Inhibition of Akt(s473) phosphorylation 23341541
Granta-519 Function Assay 1 μM 2 h Inhibition of Akt(t308) phosphorylation 23341541
JEKO-1 Function Assay 1 μM 72 h Inhibition of Akt phosphorylation in IgM-stimulated JEKO-1 23341541
Primary CLL cell Function Assay 1 μM 15 min Blocks BCR-induced LCP1 serine-5 activation 24009233
Microglia Function Assay 5 μM 10 h Decrease of TNFa secretion from LPS-stimulated p110δD910A/D910A microglia 24625684
Primary AML cell Growth Inhibition Assay 1 μM 3 h Suppression of rRNA synthesis 25014775
Primary AML cell Function Assay 1 μM 3 h Inhibition of GSK3 phosphorylation 25014775
Primary AML cell Function Assay 1 μM 3 h Inhibition of P70S6K phosphorylation 25014775
Primary AML cell Function Assay 1 μM 3 h Inhibition of Akt phosphorylation 25014775
K562 Growth Inhibition Assay 1 μM 72 h Inhibition of proliferation 25014775
K562 Function Assay 1 μM 3 h Inhibition of GSK3 phosphorylation 25014775
K562 Function Assay 1 μM 3 h Inhibition of P70S6K phosphorylation 25014775
K562 Function Assay 1 μM 3 h Inhibition of Akt phosphorylation 25014775
U266 Growth Inhibition Assay 40 μM 48 h 79.5% inhibition rate 25339332
HuT78 Growth Inhibition Assay 10 μM 72 h does not induce apoptosis 22801959
MJ Growth Inhibition Assay 10 μM 72 h does not induce apoptosis 22801959
DERL7 Growth Inhibition Assay 10 μM 72 h does not induce apoptosis 22801959
L1236 Function Assay 10 μM 2 h Inhibition of Akt phosphorylation 22210877
L428 Function Assay 10 μM 2 h Inhibition of Akt phosphorylation 22210877
L591 Function Assay 10 μM 2 h Inhibition of Akt phosphorylation 22210877
KMH-2 Function Assay 10 μM 2 h Inhibition of Akt phosphorylation 22210877
L1236 Function Assay 5 μM 24 h Blocks secretion of the CCL5 22210877
L591 Function Assay 5 μM 24 h Blocks secretion of the CCL5 22210877
L1236 Apoptosis Assay 5 μM 24 h Induction of apoptosis 22210877
L591 Apoptosis Assay 5 μM 24 h Induction of apoptosis 22210877
U-87MG Function Assay 100 nM 24 h Inhibition of cell migration 22079609
SW1783 Function Assay 100 nM 24 h Inhibition of cell migration 22079609
U-87MG Function Assay 5 μM 24 h Inhibition of Akt phosphorylation substantially 22079609
SW1783 Function Assay 5 μM 24 h Inhibition of Akt phosphorylation substantially 22079609
U-373MG Function Assay 5 μM 24 h Inhibition of Akt phosphorylation substantially 22079609
SK-MG3 Function Assay 5 μM 24 h Inhibition of Akt phosphorylation substantially 22079609
SU-DHL-5 Function Assay 1 μM 24 h Induction of apoptosis 20959606
WSU-NHL Function Assay 1 μM 24 h Induction of apoptosis 20959606
CCRF-SB Function Assay 1 μM 24 h Induction of apoptosis 20959606
INA-6 Function Assay 5 μM 6 h Inhibition of PI3K/Akt and ERK pathway 20505158
LB Function Assay 5 μM 6 h Inhibition of PI4K/Akt and ERK pathway 20505158
MOLM14 Antitumor assay 100 mg/kg 14 days Antitumor activity against human MOLM14 cells xenografted in nu/nu mouse assessed as tumor growth inhibition at 100 mg/kg, po administered daily via gavage dosed for 14 days and measured daily during compound dosing relative to control 30053721
MOLM14 Antitumor assay 100 mg/kg 14 days Antitumor activity against human MOLM14 cells xenografted in nu/nu mouse assessed as induction of apoptosis at 100 mg/kg, po administered daily via gavage dosed for 14 days and measured daily during compound dosing by TUNEL based assay 30053721
MOLM14 Antitumor assay 100 mg/kg 14 days Antitumor activity against human MOLM14 cells xenografted in nu/nu mouse assessed as inhibition of tumor proliferation 100 mg/kg, po administered daily via gavage dosed for 14 days and measured daily during compound dosing by Ki-67 labelling based immunoh 30053721
MOLM14 Antiproliferative assay 3 days Antiproliferative activity against human MOLM14 cells after 3 days by CellTiter-Glo assay, IC50 = 3.6 μM. 27774127
MV4-11 Antiproliferative assay 3 days Antiproliferative activity against human MV4-11 cells after 3 days by CellTiter-Glo assay, IC50 = 6.3 μM. 27774127
Jurkat Antiproliferative assay 3 days Antiproliferative activity against human Jurkat cells after 3 days by CellTiter-Glo assay, IC50 = 7.9 μM. 27774127
Loucy Antiproliferative assay 3 days Antiproliferative activity against human Loucy cells after 3 days by CellTiter-Glo assay, IC50 = 8.4 μM. 27774127
MOLT4 Antiproliferative assay 3 days Antiproliferative activity against human MOLT4 cells after 3 days by CellTiter-Glo assay, IC50 = 10.6 μM. 27774127
SUDHL6 Antiproliferative assay 72 hrs Antiproliferative activity against human SUDHL6 cells measured after 72 hrs by alamar blue assay, IC50 = 0.1176 μM. 27846451
SU-DHL4 Antiproliferative assay 72 hrs Antiproliferative activity against human SU-DHL4 cells measured after 72 hrs by alamar blue assay, IC50 = 1.6 μM. 27846451
Pfeiffer Antiproliferative assay 72 hrs Antiproliferative activity against human Pfeiffer cells measured after 72 hrs by alamar blue assay, IC50 = 6.8 μM. 27846451
KARPAS422 Antiproliferative assay 72 hrs Antiproliferative activity against human KARPAS422 cells measured after 72 hrs by alamar blue assay, IC50 = 8.1 μM. 27846451
Sf21 Function assay 30 mins Inhibition of N-terminal His6-tagged recombinant full-length human PI3K p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2/ATP as substrate after 30 mins by TR-FRET assay, IC50 = 3.7 μM. 28106991
Sf21 Function assay 30 mins Inhibition of N-terminal His6-tagged recombinant full-length human PI3K p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2/ATP as substrate after 30 mins by TR-FRET assay, IC50 = 3.7 μM. 28106991
RPMI8266 Antiproliferative assay 72 hrs Antiproliferative activity against human RPMI8266 cells after 72 hrs by MTT assay, IC50 = 0.00549 μM. 28325601
Raji Antiproliferative assay 72 hrs Antiproliferative activity against human Raji cells after 72 hrs by MTT assay, IC50 = 0.00995 μM. 28325601
SUDHL6 Antiproliferative assay 72 hrs Antiproliferative activity against human SUDHL6 cells after 72 hrs by CCK8 assay, IC50 = 0.65 μM. 29534936
RPMI8226 Antiproliferative assay 72 hrs Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay, IC50 = 5.49 μM. 29534936
Raji Antiproliferative assay 72 hrs Antiproliferative activity against human Raji cells after 72 hrs by MTT assay, IC50 = 9.95 μM. 29534936
MOLM13 Growth inhibition assay 72 hrs Growth inhibition of human MOLM13 cells after 72 hrs by CellTiter-Glo luminescent assay, GI50 = 1.7 μM. 30053721
MOLM14 Growth inhibition assay 72 hrs Growth inhibition of human MOLM14 cells after 72 hrs by CellTiter-Glo luminescent assay, GI50 = 6.4 μM. 30053721
CLL PBMCs Growth Inhibition Assay IC50=2.9 nM 25917267
MEC1 Growth Inhibition Assay IC50=20.4 μM 25999352
B-cells Function assay Inhibition of PI3Kdelta in B-cells by proliferation assay, IC50 = 0.0061 μM. 22924688
insect cells Function assay Inhibition of recombinant human full length His-tagged PI3Kgamma expressed in insect cells, IC50 = 0.089 μM. 27846451
insect cells Function assay Inhibition of recombinant human full length His-tagged PI3Kbeta expressed in insect cells, IC50 = 0.565 μM. 27846451
KARPAS422 Growth inhibition assay Growth inhibition of human KARPAS422 cells by CCK8 assay, GI50 = 0.68 μM. 28835805
Pfeiffer Growth inhibition assay Growth inhibition of human Pfeiffer cells by CCK8 assay, GI50 = 0.74 μM. 28835805
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
SU-DHL6 Growth inhibition assay Growth inhibition of human SU-DHL6 cells by CellTiter-Glo assay, GI50 = 0.042 μM. 29601991
点击查看更多细胞系数据

生物活性

产品描述 Idelalisib (CAL-101)是选择性p110δ抑制剂，在无细胞试验中IC50为 2.5 nM；对 p110δ 表现出的选择性是对 p110α/β/γ 的 40 到 300 倍，对p110δ的选择性是对 C2β，hVPS34，DNA-PK 和 mTOR的400到4000倍。Idelalisib 还可诱导自噬。
特性 Calistoga 暗示 CAL-101治疗血液恶性肿瘤可能有更广泛的应用价值。
靶点
p110δ [1]
(Cell-free assay)		 p110γ [1]
(Cell-free assay)
2.5 nM 89 nM
体外研究(In Vitro)
体外研究活性

CAL-101 对p110α, p110β,和p110γ作用效果不大。CAL-101作用于原代嗜碱细胞特定阻断FcϵR1 p110δ调节的 CD63表达，EC50 为8 nM。与急性髓性白血病(AML) 和骨髓增生性肿瘤(MPN) 细胞相比，CAL-101 作用于B-cell急性淋巴细胞白血病(B-ALL)和慢性淋巴细胞白血病(CLL) 细胞时显示更强的活性。CAL-101 作用于SU-DHL-5, KARPAS-422 和CCRF-SB细胞，降低pAktS473, pAktT308, 和下游靶点S6， EC50为0.1到1.0 μM。 [1]

CAL-101 作用于CLL细胞，诱导选择性细胞毒性，不是通过突变状态或间期细胞遗传学,主要通过caspase依赖机制。与正常B细胞相比，CAL-101作用于CLL 细胞优先产生细胞毒性，和LY294002相比，作用于其他造血细胞不会产生毒性。CAL-101 作用于T 细胞和天然杀伤细胞 缺乏直接的细胞毒性潜能。CAL-101抑制炎症细胞因子的产生,比如 IL-6, IL-10, TNF-α,和IFN-γ,且激活诱导的细胞因子,如CD40L。CAL-101 也抗CD40L调节的CLL细胞存活。[2]

CAL-101 作用于L1236和L591细胞, 诱导细胞在G1期积累，在S期下降，说明 CAL-101可以作为治疗霍杰金淋巴瘤(HL)的一种新策略。[3]
激酶实验 PI3K实验
用全CLL和正常B细胞溶解物进行PI3K实验。 进行PI3K ELISA 实验。全细胞抽提物加到PI(4,5)P2 底物和反应 buffer（包含 ATP)的混合物中，在室温下温育。加入 PI(3,4,5)P3 探测器和 EDTA混合，反应终止，在室温下温育1小时。混合物转移到PI3K ELISA板上，再温育1小时。 冲洗反应板，然后和第二探测器再温育30分钟。再次冲洗反应板, 加入3,3′,5,5′-四甲基联苯胺溶液 ，反应5分钟，加入H2SO4 终止反应。在450纳米处读数。
细胞实验 细胞系 CLL B 细胞或健康志愿者的T细胞或NK细胞
浓度 0.01-100 μM
孵育时间 48小时
方法

进行MTT实验测定细胞毒性。1×105个细胞和CAL-101一起温育。加入MTT试剂, 再次温育20小时，然后用溶于PBS的硫酸鱼精蛋白冲洗。加入DMSO, 用分光光度计在540纳米处测定吸光度。使用膜联蛋白/PI液式细胞计检查在不同时间点测定细胞存活力，分析数据。每个样本至少计数104个细胞。以全部阳性细胞与未处理细胞之比百分数的形式来表示实验结果。加入100 μM Z-VAD检测caspase-依赖的细胞凋亡。加入 1 μg/mL CD40L, 800 U/mL IL-4, 50 ng/mL BAFF, 20 ng/mL TNF-α测定存活信号, 或者共培养在纤连蛋白或 HS-5 细胞系基质包被的板上。 基质共培养 在75cm2培养瓶 (80%-100% 融合率) 培养24 小时，然后加入CLL细胞。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot PUMA / p53 Bim / Bcl-xl / Bid / Mcl-1 p-p65 p-AKT / AKT Cleaved caspase 3 / Cleaved caspase 9 Mcl-1 / Bcl-2 / Bid / Bcl-xl / Noxa / Bak / Bax p-FoxO3a / FoxO3a Akt(T308) / PDK1(S241) / GSK-3β(S9) 28008149
Growth inhibition assay Cell viability Cell viability 28008149
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03582098 Completed
Chronic Lymphocytic Leukaemia
Gilead Sciences
 September 12 2018 --
NCT03151057 Terminated
B Cells-Tumors|B Cell Chronic Lymphocytic Leukemia|Follicular Lymphoma|Mantle Cell Lymphoma|Large B-Cell Diffuse Lymphoma of Bone (Diagnosis)
Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Gilead Sciences
 July 31 2018 Phase 1
NCT03568929 Completed
Follicular Non-Hodgkin''s Lymphoma Refractory
Gilead Sciences
 May 25 2018 --
  • https://pubmed.ncbi.nlm.nih.gov/20959606/
  • https://pubmed.ncbi.nlm.nih.gov/20522708/
  • https://pubmed.ncbi.nlm.nih.gov/22210877/
  • https://pubmed.ncbi.nlm.nih.gov/24625684/

化学信息&溶解度

分子量 415.42 分子式

C22H18FN7O
CAS号 870281-82-6 SDF Download Idelalisib (CAL-101) SDF
Smiles CCC(C1=NC2=C(C(=CC=C2)F)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5
储存条件(自收到货起)

体外溶解度
批次：

DMSO : 83 mg/mL ( (199.79 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解配方
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

 动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器（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）

mg/kg g μL 只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

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，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

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。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 1:
What is the recommended dose of CAL-101 and the route of administration for mouse studies?

回答：
According to the following paper, S2226 can be used by I.V. administration at the concentration of 40 mg/kg. https://www.ncbi.nlm.nih.gov/pubmed/24625684

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