2. PI3K/Akt/mTOR Apoptosis
  3. PI3K Apoptosis
  4. PI3Kδ/γ-IN-3

PI3Kδ/γ-IN-3 (Compound 58) 是一种口服有效的 PI3Kδ 和 PI3Kγ 双抑制剂，IC50 值分别为 1 nM 和 16 nM。 PI3Kδ/γ-IN-3 诱导肿瘤细胞凋亡（apoptosis），可用于 B 细胞恶性肿瘤的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PI3Kδ/γ-IN-3 Chemical Structure

PI3Kδ/γ-IN-3 Chemical Structure

CAS No. : 2730151-31-0

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

PI3Kδ/γ-IN-3 相关抗体

Top Publications Citing Use of Products

查看 PI3K 亚型特异性产品:

查看所有亚型
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3Kδ/γ-IN-3 (Compound 58) is a potent and orally active PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 16 nM, respectively. PI3Kδ/γ-IN-3 induces tumor cell apoptosis and can be used for B-cell malignancies research[1].

IC50 & Target

PI3Kδ

1 nM (IC50)

PI3Kγ

16 nM (IC50)

体外研究
(In Vitro)

PI3Kδ/γ-IN-3 (Compound 58) (72 h) shows antiproliferative activity against B-cell lymphoma (DLBCL) cells[1].
PI3Kδ/γ-IN-3 (0.5 μM, 24 h) arrests cell cycle at G0/G1 phase in SUDHL-6 and DOHH2 cells[1].
PI3Kδ/γ-IN-3 (1.5 and 2 μM, 48 h) induces cell apoptosis in SUDHL-6 and DOHH2 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PI3Kδ/γ-IN-3 相关抗体:

Cell Proliferation Assay[1]

Cell Line: SUDHL-4, SUDHL-6 and DOHH2 cells
Concentration:
Incubation Time: 72 h
Result: Showed antiproliferative activity with IC50s of 0.03 ± 0.03, 0.06 ± 0.01 and 0.20 ± 0.04 μM against SUDHL-4, SUDHL-6 and DOHH2 cells, respectively.

Cell Cycle Analysis[1]

Cell Line: SUDHL-6 and DOHH2 cells
Concentration: 0.5 μM
Incubation Time: Alone or in combination with Ibrutininb (HY-10997) (0.5 μM or 1 μM) for 24 h
Result: Caused a loss of G2/M phase cells and an increase in the percentage of cells in the G0/G1 phase. Induced cell cycle arrest alone or in combination with Ibrutinib in both cells.

Apoptosis Analysis[1]

Cell Line: SUDHL-6 and DOHH2 cells
Concentration: 1.5 μM and 2 μM
Incubation Time: Alone or in combination with Ibrutininb (1.5 μM or 1 μM) for 48 h
Result: Demonstrated the induction of apoptosis in both SUDHL-6 and DOHH2 cells, and the combination was stronger than treated alone.
体内研究
(In Vivo)

PI3Kδ/γ-IN-3 (Compound 58) (5 and 10 mg/kg; p.o.; daily for 14d) suppresses the tumor volume in a dose-dependent manner without obvious toxicity in mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female non obese diabetes/severe combined immunodeficient (NOD/SCID) mice, 6- to 8-week-old, SUDHL-6 xenograft model[1]
Dosage: 5 and 10 mg/kg alone or in combination with 10 mg/kg Ibrutinib
Administration: Oral administration, daily for 14 days
Result: Suppressed the tumor volume in a dose-dependent manner and demonstrated superior efficacy relative to Ibrutinib at 10 mg/kg QD administration. When in combination with Ibrutinib, showed greater tumor growth inhibitory effects.
Animal Model: SD rats[1]
Dosage: 5 mg/kg
Administration: Oral or intravenous administration (Pharmacokinetic Analysis)
Result: PK Profiles of PI3Kδ/γ-IN-3 (Compound 58) in Male SD Rats[1]
Compound dose (mg/kg) administration route Cmax (ng/mL) Tmax (h) AUC0-t (h•μg/L) T1/2 (h) CL (L/h/kg) Vss(L/kg) F (%)
58 5 oral 3637.81 3.33 8612.57 9.46 0.79 -- 126.5
5 intravenous 860.09 0.08 6806.92 2.79 0.75 2.86 --

PK profiles: Cmax, maximum plasma concentration; Tmax, tim
分子量

473.92

Formula

C23H20ClN9O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PI3Kδ/γ-IN-3 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PI3Kδ/γ-IN-32730151-31-0PI3KApoptosisPhosphoinositide 3-kinaseB-cell malignanciesDLBCLIbrutinibSUDHL-6DOHH2Inhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
PI3Kδ/γ-IN-3
目录号：
HY-150638
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z