Serabelisib | MLN1117 | p110α Inhibitor | AmBeed-信号通路专用抑制剂

Serabelisib {[allProObj[0].p_purity_real_show]}

货号：A446445 同义名： MLN1117; INK1117

Serabelisib是一种选择性的 p110α 抑制剂，IC50 为 15 nM。

Serabelisib 化学结构
CAS号：1268454-23-4

Serabelisib 3D分子结构
CAS号：1268454-23-4

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PI3K 亚型比较

产品名称	C2β ↓ ↑	p110α ↓ ↑	p110β ↓ ↑	p110γ ↓ ↑	p110δ ↓ ↑	PI3K ↓ ↑	Vps34 ↓ ↑	其他靶点	纯度
A66	+ C2β, IC50: 462 nM	++ p110α, IC50: 32 nM							99%+
Taselisib	+ C2β, IC50: 292 nM	++++ PI3Kα, Ki: 0.29 nM	+++ PI3Kβ, Ki: 9.1 nM	++++ PI3Kγ, Ki: 0.97 nM	++++ PI3Kδ, Ki: 0.12 nM		+ hVps34, IC50: 374 nM		99%+
Gedatolisib		++++ PI3Kα, IC50: 0.4 nM		+++ PI3Kγ, IC50: 5.4 nM				mTOR	99%
HS-173		++++ PI3Kα , IC50: 0.8 nM							99%+
Serabelisib		+++ PI3Kα, IC50: 21 nM							99%+
GNE-477		++++ PI3Kα, IC50: 4 nM						mTOR	99%
YM-201636		+ p110α, IC50: 3.3 μM						PIKfyve	98%
AS-252424		+ PI3Kα, IC50: 935 nM		++ PI3Kγ, IC50: 33 nM					99%
Alpelisib		+++ PI3Kα, IC50: 5 nM							99%+
AS-604850		+ PI3Kα, IC50: 4.5 μM		+ PI3Kγ, IC50: 0.25 μM					99%
SF2523		++ PI3Kα, IC50: 34 nM		++ PI3Kγ, IC50: 158 nM				DNA-PK,mTOR	99%+
Inavolisib		++++ PI3K alpha, IC50: 0.038 nM							99%+
Bimiralisib		++++ PI3Kα, Kd: 1.5 nM	+++ PI3Kβ, Kd: 11 nM	++ PI3Kγ, Kd: 25 nM	++ PI3Kδ, Kd: 25 nM			mTOR	99%+
GSK1059615		++++ PI3Kα, IC50: 0.4 nM	++++ PI3Kβ, IC50: 0.6 nM	+++ PI3Kγ, IC50: 5 nM	++++ PI3Kδ, IC50: 2 nM			mTOR	98%
GSK2636771			✔						99%
Fimepinostat		+++ PI3Kα, IC50: 19 nM	++ PI3Kβ, IC50: 54 nM		++ PI3Kδ, IC50: 39 nM				99%+
VS-5584		++++ PI3Kα, IC50: 2.6 nM	+++ PI3Kβ, IC50: 21 nM	++++ PI3Kγ, IC50: 3.0 nM	++++ PI3Kδ, IC50: 2.7 nM			mTOR	98%
Dactolisib		++++ p110α1, IC50: 4 nM	++ p110β, IC50: 75 nM	+++ p110γ, IC50: 5 nM	+++ p110δ, IC50: 7 nM				98+%
PI-103		++++ p110α, IC50: 2 nM	++++ p110β, IC50: 3 nM	+++ p110γ, IC50: 15 nM	++++ p110δ, IC50: 3 nM			DNA-PK,mTOR	99%+
PI-3065			+ p110β, IC50: 1078 nM		+++ p110δ, IC50: 15 nM				99%+
Voxtalisib		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	99%+
AZD-8835		+++ PI3Kα, IC50: 6.2 nM	+ PI3Kβ, IC50: 431 nM	++ PI3Kγ, IC50: 90 nM	+++ PI3Kδ, IC50: 5.7 nM				99%
Pilaralisib analogue		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 36 nM	+++ PI3Kγ, IC50: 23 nM	++ PI3Kδ, IC50: 36 nM				99%+
ZSTK474		+++ PI3Kα, IC50: 16 nM	++ PI3Kβ, IC50: 44 nM	++ PI3Kγ, IC50: 49 nM	+++ PI3Kδ, IC50: 4.6 nM	++ PI3K, IC50: 37 nM			98%
AS-605240		++ PI3Kα, IC50: 60 nM	+ PI3Kβ, IC50: 270 nM	+++ PI3Kγ, IC50: 8 nM	+ PI3Kδ, IC50: 300 nM				98%
TGX-221			+++ p110β, IC50: 5 nM		++ p110δ, IC50: 0.1 μM				99%+
PF-04691502		++++ PI3Kα, Ki: 1.8 nM	++++ PI3Kβ, Ki: 2.1 nM	++++ PI3Kγ, Ki: 1.9 nM	++++ PI3Kδ, Ki: 1.6 nM			mTOR	98+%
GDC-0084		++++ PI3Kα, Ki app: 2 nM	++ PI3Kβ, Ki app: 46 nM	+++ PI3Kγ, Ki app: 10 nM	++++ PI3Kδ, Ki app: 3 nM			mTOR	99%+
Buparlisib		++ p110α, IC50: 52 nM	+ p110β, IC50: 166 nM	+ p110γ, IC50: 262 nM	++ p110δ, IC50: 116 nM		+ Vps34, IC50: 2.4 μM	mTOR	98%
LY294002		+ p110α, IC50: 0.5 μM	+ p110β, IC50: 0.97 μM		+ p110δ, IC50: 0.57 μM			DNA-PK	99%+
AZD 6482		+ PI3Kα, IC50: 870 nM	+++ PI3Kβ, IC50: 10 nM		++ PI3Kδ, IC50: 80 nM			DNA-PK	99%+
Pictilisib		++++ p110α, IC50: 3 nM	++ p110β, IC50: 33 nM	++ p110γ, IC50: 75 nM	++++ p110δ, IC50: 3 nM			mTOR	99%+
PKI-402		++++ PI3Kα, IC50: 2 nM	+++ PI3Kβ, IC50: 7 nM	+++ PI3Kγ, IC50: 16 nM	+++ PI3Kδ, IC50: 14 nM			mTOR	98%
Copanlisib		++++ PI3Kα, IC50: 0.5 nM	++++ PI3Kβ, IC50: 3.7 nM	+++ PI3Kγ, IC50: 6.4 nM	++++ PI3Kδ, IC50: 0.7 nM				99%+
Omipalisib		++++ p110α, Ki: 0.019 nM	++++ p110β, Ki: 0.13 nM	++++ p110γ, Ki: 0.06 nM	++++ p110δ, Ki: 0.024 nM				99%+
Izorlisib		+++ PI3Kα, IC50: 14 nM	++ PI3Kβ, IC50: 0.12 μM	++ PI3Kγ, IC50: 36 nM	+ PI3Kδ, IC50: 0.50 μM				99%+
AZD8186		++ PI3Kα, IC50: 35 nM	++++ PI3Kβ, IC50: 4 nM		+++ PI3Kδ, IC50: 12 nM				99%
KU-0060648		++++ PI3Kα, IC50: 4 nM	++++ PI3Kβ, IC50: 0.5 nM	+ PI3Kγ, IC50: 0.59 μM	++++ PI3Kδ, IC50: 0.1 nM			DNA-PK	98%
Apitolisib		+++ p110α, IC50: 5 nM	++ p110β, IC50: 27 nM	+++ p110γ, IC50: 14 nM	+++ p110δ, IC50: 7 nM			mTOR	98%+
CZC24832			+ PI3Kβ, IC50: 1.1 μM	++ PI3Kγ, IC50: 27 nM					98+%
BGT226 maleate		++++ PI3Kα, IC50: 4 nM	++ PI3Kβ, IC50: 63 nM	++ PI3Kγ, IC50: 38 nM				mTOR	99%+
TG 100713		++ PI3Kα, IC50: 165 nM	+ PI3Kβ, IC50: 215 nM	++ PI3Kγ, IC50: 50 nM	+++ PI3Kδ, IC50: 24 nM				98%+
PI3K-IN-1		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	98+%
TG100-115		+ PI3Kα, IC50: 1.3 μM	+ PI3Kβ, IC50: 1.2 μM	++ PI3Kγ, IC50: 83 nM	+ PI3Kδ, IC50: 235 nM				98%
PIK-90		+++ PI3Kα, IC50: 11 nM	+ PI3Kβ, IC50: 350 nM	+++ PI3Kγ, IC50: 18 nM	++ PI3Kδ, IC50: 58 nM				99%+
PIK-294			+ p110β, IC50: 490 nM	++ p110γ, IC50: 160 nM	+++ p110δ, IC50: 10 nM				99%+
Duvelisib			++++ PI3Kβ, Ki: 1564 pM	++ PI3Kγ, Ki: 243 pM	++++ PI3Kδ, Ki: 23 pM				99%+
GDC-0326		++++ PI3Kα, Ki: 0.2 nM	++ PI3Kβ, Ki: 26.6 nM	+++ PI3Kγ, Ki: 10.2 nM	++++ PI3Kδ, Ki: 4 nM				98%
Quercetin Dihydrate			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM				95%
Quercetin			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM			Sirtuin,PKC,Src	95%
Leniolisib		+ PI3Kα, IC50: 0.244 μM	+ PI3Kβ, IC50: 0.424 μM	+ PI3Kγ, IC50: 2.23 μM	+++ PI3Kδ, IC50: 0.011 μM			DNA-PK	99%+
PIK-108			✔						99%
Eganelisib				+++ PI3Kγ, IC50: 16 nM					99%+
CAY10505				✔					99%
IPI-3063					++++ p110δ, IC50: 2.5 nM				99%
Nemiralisib					++++ PI3Kδ, pKi: 9.9				99%+
PF-4989216		++++ p110α, IC50: 2 nM		++ p110γ, IC50: 65 nM	++++ p110δ, IC50: 1 nM				99%+
PIK-75 HCl		+++ p110α, IC50: 5.8 nM		++ p110γ, IC50: 76 nM	+ p110δ, IC50: 0.51 μM			DNA-PK	99%+
Tenalisib				++ PI3Kγ, IC50: 33.2 nM	++ PI3Kδ, IC50: 24.5 nM				98%
Acalisib					+++ p110δ, IC50: 14 nM				99%+
Umbralisib					+++ PI3Kδ, IC50: 22.2 nM				99%+
AMG319				+ PI3Kγ, IC50: 850 nM	+++ PI3Kδ, IC50: 18 nM				99%
IC-87114				+ PI3Kγ, IC50: 29 μM	+ PI3Kδ, IC50: 0.5 μM				99%+
Idelalisib				++ p110γ, IC50: 89 nM	++++ p110δ, IC50: 2.5 nM				98%
PIK-293				+ p110γ, IC50: 10 μM	+ p110δ, IC50: 0.24 μM				99%+
Vps34-PIK-III					+ PI3Kδ, IC50: 1.2μM		+++ Vps34, IC50: 0.018μM		99%+
GSK2292767					✔				98%
Seletalisib				+ PI3Kγ, IC50: 282 nM	+++ PI3Kδ, IC50: 12 nM				99%+
P110δ-IN-1					++++ P110δ, IC50: 0.6 nM				99%
PI3Kδ-IN-5					++++ PI3Kδ, IC50: 0.9 nM				99%
SRX3207		+ PI3K alpha, IC50: 244 nM		+ PI3K gamma, IC50: 9790 nM	+ PI3K delta, IC50: 388 nM			Syk	98%
Parsaclisib HCl					++++ PI3Kδ, IC50: 1 nM				98%
IHMT-PI3Kδ-372					+++ PI3Kδ, IC50: 14 nM				98%
Trigonelline						✔		Akt	99%+
Wortmannin						++++ PI3K, IC50: 3 nM		DNA-PK,MLCK	99%+
Samotolisib						✔		DNA-PK	99%+
GNE-317						✔			99%+
Oroxin B						✔		Akt,PTEN	99%+
NU 7026						+ PI3K, IC50: 13 μM		DNA-PK	98+%
Deguelin						✔		Akt	99%+
Ailanthone						✔		CDK,Akt,ATM/ATR	98%
Resibufogenin						✔		ROS	98%
KU-57788						+ PI3K, IC50: 5 μM		DNA-PK,mTOR	99%+
Cinobufagine						✔		Akt	99%
α-Linolenic acid						✔			97% (GC)
MTX-211						✔		EGFR	98%
PI3K/mTOR Inhibitor-2						++++ PI3K, IC50: 3.4 nM		mTOR	99%+
SPP-86						✔			99%+
(E)-Akt inhibitor-IV						✔			98%
Vps34-IN-1							++ Vps34, IC50: 25 nM		98%
SAR405							++++ Vps34, IC50: 1.2 nM		98+%
3-Methyladenine				+ PI3Kγ, IC50: 60 μM			+ Vps34, IC50: 25 μM	Autophagy	98%
Vps34-IN-4							+++ VPS34, IC50: 15 nM		98%+
Autophinib							+++ Vps34, IC50: 19 nM	Autophagy	99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Serabelisib 生物活性

靶点

p110α

PI3Kα, IC50:21 nM

描述

The PI3K pathway is a frequently dysregulated signaling cascade in human cancer. Activating mutations in PIK3CA (encoding the p110α catalytic subunit of PI3Kα) are strongly implicated in oncogenic PI3K signaling. MLN1117 is a potent and selective oral PI3Kα isoform inhibitor (IC₅₀ of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinases. MLN1117 administration in PIK3CA-mutant tumor cell lines resulted in potent PI3K pathway inhibition, blockade of cellular proliferation, and apoptosis. MLN1117 (100 – 1200 mg) exhibited moderately fast oral absorption, a generally dose proportional increase in exposure, and plasma half-life of approximately 11 hours. Preclinical studies showed MLN1117 to have low potential for disrupting glucose metabolism or for causing cardiac adverse events; in rats and monkeys, doses up to 50 mg/kg/day were well tolerated. Administration of MLN1117 also led to dose-dependent inhibition of tumor growth in murine xenograft models of human cancer (e.g., breast carcinoma) bearing PIK3CA oncogenic mutations, with corresponding inhibition of PI3K pharmacodynamic markers in tumor tissue^[3].

Serabelisib 细胞实验

Cell Line CRL-2396 Jurkat TIB-48 B cells U87MG cells SK-OV-3 cells	Concentration	Treated Time	Description	References
CRL-2396	21.37μM		Evaluate the inhibitory activity of MLN1117 on CRL-2396 cells	Oncotarget. 2017 Nov 1;8(59):100326-100338.
Jurkat	36.45μM		Evaluate the inhibitory activity of MLN1117 on Jurkat cells	Oncotarget. 2017 Nov 1;8(59):100326-100338.
TIB-48	9.75μM		Evaluate the inhibitory activity of MLN1117 on TIB-48 cells	Oncotarget. 2017 Nov 1;8(59):100326-100338.
B cells	1 μM	3 days	Evaluate the effect of MLN1117 on B cell proliferation, results showed 1 μM MLN1117 had no significant effect on B cell proliferation	J Biol Chem. 2013 Feb 22;288(8):5718-31.
U87MG cells	125 nM to 2 μM	48 hours	Evaluate the effect of MLN1117 on U87MG cell growth, results showed MLN1117 had no significant effect on cell growth at concentrations from 125 nM to 2 μM	J Biol Chem. 2013 Feb 22;288(8):5718-31.
SK-OV-3 cells	125 nM to 2 μM	48 hours	Evaluate the effect of MLN1117 on SK-OV-3 cell growth, results showed MLN1117 significantly inhibited cell growth at concentrations from 125 nM to 2 μM	J Biol Chem. 2013 Feb 22;288(8):5718-31.

Cell Line

CRL-2396 Jurkat TIB-48 B cells U87MG cells SK-OV-3 cells

Concentration

Treated Time

Description

References

CRL-2396

21.37μM

Evaluate the inhibitory activity of MLN1117 on CRL-2396 cells

Oncotarget. 2017 Nov 1;8(59):100326-100338.

Jurkat

36.45μM

Evaluate the inhibitory activity of MLN1117 on Jurkat cells

Oncotarget. 2017 Nov 1;8(59):100326-100338.

TIB-48

9.75μM

Evaluate the inhibitory activity of MLN1117 on TIB-48 cells

Oncotarget. 2017 Nov 1;8(59):100326-100338.

B cells

1 μM

3 days

Evaluate the effect of MLN1117 on B cell proliferation, results showed 1 μM MLN1117 had no significant effect on B cell proliferation

J Biol Chem. 2013 Feb 22;288(8):5718-31.

U87MG cells

125 nM to 2 μM

48 hours

Evaluate the effect of MLN1117 on U87MG cell growth, results showed MLN1117 had no significant effect on cell growth at concentrations from 125 nM to 2 μM

J Biol Chem. 2013 Feb 22;288(8):5718-31.

SK-OV-3 cells

125 nM to 2 μM

48 hours

Evaluate the effect of MLN1117 on SK-OV-3 cell growth, results showed MLN1117 significantly inhibited cell growth at concentrations from 125 nM to 2 μM

J Biol Chem. 2013 Feb 22;288(8):5718-31.

Serabelisib 动物实验

Species Mice Mice BALB/c mice	Animal Model Balb/cJ mice C57BL/6 mice PTCL xenograft model	Administration	Dosage	Frequency	Description	References
Mice	Balb/cJ mice	Oral gavage	60 mg/kg	Daily administration for 13 days	Evaluate the effect of MLN1117 on immune responses in mice, results showed 60 mg/kg MLN1117 did not affect NP-specific IgM or IgG1 responses	J Biol Chem. 2013 Feb 22;288(8):5718-31.
Mice	C57BL/6 mice	Oral	60 mg/kg	Once daily for 7 days	To evaluate the effect of MLN1117 on NK cell maturation and function. Results showed that MLN1117 had negligible effects on NK subset maturation or terminal subset commitment.	PLoS One. 2014 Jun 10;9(6):e99486.
BALB/c mice	PTCL xenograft model	Oral	30 mg/kg	Once daily for 3 weeks	Evaluate the anti-tumor activity of alisertib combined with MLN1117 in a PTCL xenograft model, showing significant tumor growth inhibition	Oncotarget. 2017 Nov 1;8(59):100326-100338.

Species

Mice Mice BALB/c mice

Animal Model

Balb/cJ mice C57BL/6 mice PTCL xenograft model

Administration

Dosage

Frequency

Description

References

Mice

Balb/cJ mice

Oral gavage

60 mg/kg

Daily administration for 13 days

Evaluate the effect of MLN1117 on immune responses in mice, results showed 60 mg/kg MLN1117 did not affect NP-specific IgM or IgG1 responses

J Biol Chem. 2013 Feb 22;288(8):5718-31.

Mice

C57BL/6 mice

Oral

60 mg/kg

Once daily for 7 days

To evaluate the effect of MLN1117 on NK cell maturation and function. Results showed that MLN1117 had negligible effects on NK subset maturation or terminal subset commitment.

PLoS One. 2014 Jun 10;9(6):e99486.

BALB/c mice

PTCL xenograft model

Oral

30 mg/kg

Once daily for 3 weeks

Evaluate the anti-tumor activity of alisertib combined with MLN1117 in a PTCL xenograft model, showing significant tumor growth inhibition

Oncotarget. 2017 Nov 1;8(59):100326-100338.

Serabelisib 参考文献

Serabelisib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.75mL

0.55mL

0.28mL

13.76mL

2.75mL

1.38mL

27.52mL

5.50mL

2.75mL

Serabelisib 技术信息

CAS号	1268454-23-4
分子式	C₁₉H₁₇N₅O₃
分子量	363.37
SMILES Code	O=C(C1=CN=C2C=CC(C3=CC=C(OC(N)=N4)C4=C3)=CN21)N5CCOCC5
MDL No.	MFCD15146372

别名	MLN1117; INK1117; TAK-117
运输	蓝冰
InChI Key	BLGWHBSBBJNKJO-UHFFFAOYSA-N
Pubchem ID	70798655

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 5 mg/mL(13.76 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

Serabelisib {[allProObj[0].p_purity_real_show]}

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