Inavolisib | GDC 0077 | PI3Kα Inhibitor | AmBeed-信号通路专用抑制剂

Inavolisib {[allProObj[0].p_purity_real_show]}

货号：A723930 同义名： GDC 0077; RG6114

Inavolisib是一种口服活性的选择性PI3Kδ抑制剂，能够有效调节PI3K信号通路，适用于治疗与免疫系统相关的癌症和炎症性疾病。

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Type	HazMat fee for 500 gram (Estimated)
Excepted Quantity	USD 0.00
Limited Quantity	USD 15-60
Inaccessible (Haz class 6.1), Domestic	USD 80+
Inaccessible (Haz class 6.1), International	USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic	USD 100+
Accessible (Haz class 3, 4, 5 or 8), International	USD 200+

Inavolisib 化学结构
CAS号：2060571-02-8

Inavolisib 3D分子结构
CAS号：2060571-02-8

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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				mTOR,DNA-PK	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			mTOR,DNA-PK	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			mTOR,DNA-PK	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			mTOR,DNA-PK	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			PKC,Src,Sirtuin	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		MLCK,DNA-PK	99%+
Samotolisib						✔		DNA-PK	99%+
GNE-317						✔			99%+
Oroxin B						✔		PTEN,Akt	99%+
NU 7026						+ PI3K, IC50: 13 μM		DNA-PK	98+%
Deguelin						✔		Akt	99%+
Ailanthone						✔		Akt,ATM/ATR,CDK	98%
Resibufogenin						✔		ROS	98%
KU-57788						+ PI3K, IC50: 5 μM		mTOR,DNA-PK	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。

Inavolisib 生物活性

靶点

p110α

PI3K alpha, IC50:0.038 nM

Inavolisib 细胞实验

Cell Line SK-BR-3 or HCC1569 cells MCF-7 cells HCC1954 cells MCF7 PIK3CA E545K HCC1954 PIK3CA H1047R	Concentration	Treated Time	Description	References
SK-BR-3 or HCC1569 cells	2 µM	24 hours	To assess the effects of PI3K inhibitors on the proliferation of HCC1569 cells. Results showed that HCC1569 cells were less susceptible to inavolisib than SK-BR-3 cells.	Cancer Metab. 2025 Feb 7;13(1):6.
MCF-7 cells	0.12 µM and above	4 days	To assess the cytotoxic response of GDC-0077 in PIK3CAE545K-mutant MCF7 cells. Results showed a strong cytotoxic response at concentrations of 0.12 μmol/L and above.	Cancer Discov. 2022 Jan;12(1):204-219.
HCC1954 cells	1 µM	8 hours	To assess the effect of taselisib on p110a protein depletion in PIK3CAH1047R-mutant HCC1954 cells. Results showed dose-dependent depletion of p110a protein.	Cancer Discov. 2022 Jan;12(1):204-219.
MCF7 PIK3CA E545K	0.123 µM		Evaluate the effect of GDC-0077 in combination with palbociclib	Cancer Discov. 2022 Jan;12(1):204-219.
HCC1954 PIK3CA H1047R	0.5 µM	24 h	Assess the effect of GDC-0077 on p110a protein levels	Cancer Discov. 2022 Jan;12(1):204-219.

Cell Line

SK-BR-3 or HCC1569 cells MCF-7 cells HCC1954 cells MCF7 PIK3CA E545K HCC1954 PIK3CA H1047R

Concentration

Treated Time

Description

References

SK-BR-3 or HCC1569 cells

2 µM

24 hours

To assess the effects of PI3K inhibitors on the proliferation of HCC1569 cells. Results showed that HCC1569 cells were less susceptible to inavolisib than SK-BR-3 cells.

Cancer Metab. 2025 Feb 7;13(1):6.

MCF-7 cells

0.12 µM and above

4 days

To assess the cytotoxic response of GDC-0077 in PIK3CAE545K-mutant MCF7 cells. Results showed a strong cytotoxic response at concentrations of 0.12 μmol/L and above.

Cancer Discov. 2022 Jan;12(1):204-219.

HCC1954 cells

1 µM

8 hours

To assess the effect of taselisib on p110a protein depletion in PIK3CAH1047R-mutant HCC1954 cells. Results showed dose-dependent depletion of p110a protein.

Cancer Discov. 2022 Jan;12(1):204-219.

MCF7 PIK3CA E545K

0.123 µM

Evaluate the effect of GDC-0077 in combination with palbociclib

Cancer Discov. 2022 Jan;12(1):204-219.

HCC1954 PIK3CA H1047R

0.5 µM

24 h

Assess the effect of GDC-0077 on p110a protein levels

Cancer Discov. 2022 Jan;12(1):204-219.

Inavolisib 动物实验

Species NOD/SCID mice NCR nude mice Mice Mice	Animal Model MCF7 orthotopic xenograft model HCC1954 xenograft model HCC1954 PIK3CA H1047R xenograft model MCF7 orthotopic xenograft model	Administration	Dosage	Frequency	Description	References
NOD/SCID mice	MCF7 orthotopic xenograft model	Oral	25 mg/kg	Once daily for 28 days	To evaluate the antitumor effect of inavolisib in combination with vepdegestrant. The results showed that the combination induced tumor regression in the MCF7 xenograft model.	Clin Cancer Res. 2024 Aug 15;30(16):3549-3563.
NCR nude mice	HCC1954 xenograft model	Oral	50 mg/kg	Single dose	To assess the efficacy of GDC-0077 in depleting p110a protein in HCC1954 xenograft model. Results showed p110a protein depletion for up to 8 hours.	Cancer Discov. 2022 Jan;12(1):204-219.
Mice	HCC1954 PIK3CA H1047R xenograft model	Oral	50 mg/kg	Once daily	Evaluate the antitumor efficacy of GDC-0077 in vivo	Cancer Discov. 2022 Jan;12(1):204-219.
Mice	MCF7 orthotopic xenograft model	Oral	25 mg/kg	Once daily for 5 days, 2 days off, repeated 4 times	Inavolisib in combination with vepdegestrant showed antitumor activity in the MCF7 xenograft model, leading to tumor volume reduction.	Clin Cancer Res. 2024 Aug 15;30(16):3549-3563

Species

NOD/SCID mice NCR nude mice Mice Mice

Animal Model

MCF7 orthotopic xenograft model HCC1954 xenograft model HCC1954 PIK3CA H1047R xenograft model MCF7 orthotopic xenograft model

Administration

Dosage

Frequency

Description

References

NOD/SCID mice

MCF7 orthotopic xenograft model

Oral

25 mg/kg

Once daily for 28 days

To evaluate the antitumor effect of inavolisib in combination with vepdegestrant. The results showed that the combination induced tumor regression in the MCF7 xenograft model.

Clin Cancer Res. 2024 Aug 15;30(16):3549-3563.

NCR nude mice

HCC1954 xenograft model

Oral

50 mg/kg

Single dose

To assess the efficacy of GDC-0077 in depleting p110a protein in HCC1954 xenograft model. Results showed p110a protein depletion for up to 8 hours.

Cancer Discov. 2022 Jan;12(1):204-219.

Mice

HCC1954 PIK3CA H1047R xenograft model

Oral

50 mg/kg

Once daily

Evaluate the antitumor efficacy of GDC-0077 in vivo

Cancer Discov. 2022 Jan;12(1):204-219.

Mice

MCF7 orthotopic xenograft model

Oral

25 mg/kg

Once daily for 5 days, 2 days off, repeated 4 times

Inavolisib in combination with vepdegestrant showed antitumor activity in the MCF7 xenograft model, leading to tumor volume reduction.

Clin Cancer Res. 2024 Aug 15;30(16):3549-3563

Inavolisib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.45mL

0.49mL

0.25mL

12.27mL

2.45mL

1.23mL

24.55mL

4.91mL

2.45mL

Inavolisib 技术信息

CAS号	2060571-02-8
分子式	C₁₈H₁₉F₂N₅O₄
分子量	407.37
SMILES Code	C[C@H](NC1=CC=C2C3=NC(N4C(OC[C@H]4C(F)F)=O)=CN3CCOC2=C1)C(N)=O
MDL No.	MFCD31382124

别名	GDC 0077; RG6114; RO-7113755; GDC-0077
运输	蓝冰

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: 105 mg/mL(257.75 mM)，配合低频超声助溶，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

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

方案三

方案四

方案五

Inavolisib {[allProObj[0].p_purity_real_show]}

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Inavolisib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Inavolisib 质控信息

Inavolisib 生物活性

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Inavolisib 动物实验

Inavolisib 实验方案

Inavolisib 技术信息

最近浏览的产品

大规格询价

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