(Z)-Orantinib | SU6668 | PDGFR Inhibitor | AmBeed-信号通路专用抑制剂

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(Z)-Orantinib {[allProObj[0].p_purity_real_show]}

货号：A146183 同义名： SU6668; (Z)-TSU-68

SU6668 is a cell-permeable indolinone compound that acts as a potent ATP-competitive inhibitor against RTKs (receptor tyrosine kinases) Kit, PDGFRβ, VEGFR2 (Flk-1/KDR), FGFR1 activity in vitro (IC50 = 0.01, 0.1, 3.9, and 3.8 µM, respectively) and PDGF/VEGF/bFGF-mediated angiogenesis and tumor development. Although initially characterized as an RTK inhibitor, SU6668 is now also known to target ser/thr kinases Aurora A, Aurora B, TBK1 (NAK/T2K), and AMPK (IC50 = 0.85, 0.047, 1.4, and 1.8 µM, respectively), as well as non-receptor TKs Lyn and Yes (IC50 = 4.3 and 5.8 µM, respectively).

(Z)-Orantinib 化学结构
CAS号：210644-62-5

(Z)-Orantinib 3D分子结构
CAS号：210644-62-5

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(Z)-Orantinib 纯度/质量文件产品仅供科研

货号：A146183 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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Aurora Kinase 亚型比较
AMPK 亚型比较
NF-κB 亚型比较
VEGFR 亚型比较
c-Kit 亚型比较
PDGFR 亚型比较

产品名称	Aurora A ↓ ↑	Aurora B ↓ ↑	Aurora C ↓ ↑	其他靶点	纯度
BI-847325	++ Aurora A (Human), IC50: 25 nM	++++ Aurora B (Xenopus laevis), IC50: 3 nM	++ Aurora C (Human), IC50: 15 nM		99%+
CCT 137690	++ Aurora A, IC50: 15 nM	++ Aurora B, IC50: 25 nM	++ Aurora C, IC50: 19 nM		99%+
MK-5108	++++ Aurora A, IC50: 0.064 nM				99%+
KW-2449	+ Aurora A, IC50: 48 nM			FLT3	99%+
Tozasertib	++++ Aurora A, Ki app: 0.6 nM	++ Aurora B, Ki app: 18 nM	+++ Aurora C, Ki app: 4.6 nM	Bcr-Abl,FLT3	99%+
AT9283	++++ Aurora A, IC50: ~3.0 nM	++++ Aurora B, IC50: ~3.0 nM			99%+
MLN8054	+++ Aurora A, IC50: 4 nM	+ Aurora B, IC50: 172 nM			99%+
ZM-447439	+ Aurora A, IC50: 110 nM	+ Aurora B, IC50: 130 nM		Src	99%+
TCS7010	++++ Aurora A, IC50: 3.4 nM				99%+
TAK-901	++ Aurora A-TPX2, IC50: 21 nM	++ Aurora B-INCENP, IC50: 15 nM			99%+
Danusertib	+++ Aurora A, IC50: 13 nM	+ Aurora B, IC50: 79 nM	+ Aurora C, IC50: 61 nM	RET	99%+
MK-8745	++++ Aurora A, IC50: 0.6 nM				99+%
PHA-680632	++ Aurora A, IC50: 27 nM	+ Aurora B, IC50: 135 nM	+ Aurora C, IC50: 120 nM	FLT3	99%+
AMG 900	+++ Aurora A, IC50: 5 nM	+++ Aurora B, IC50: 4 nM	++++ Aurora C, IC50: 1 nM		99%+
Alisertib	++++ Aurora A, IC50: 1.2 nM				99%+
ENMD-2076	+++ Aurora A, IC50: 14 nM	+ Aurora B, IC50: 350 nM		FLT3,RET	98%
JNJ-7706621	+++ Aurora A, IC50: 11 nM	++ Aurora B, IC50: 15 nM			99%+
CYC-116	+++ Aurora A, Ki: 8 nM	+++ Aurora B, Ki: 9 nM		FLT3	99%+
Reversine	+++ Aurora A, IC50: 12 nM	+++ Aurora B, IC50: 13 nM	++ Aurora C, IC50: 20 nM		98%
CCT129202	++ Aurora A, IC50: 42 nM	+ Aurora B, IC50: 198 nM	+ Aurora C, IC50: 227 nM		98%
SNS-314 mesylate	+++ Aurora A, IC50: 9 nM	++ Aurora B, IC50: 31 nM	++++ Aurora C, IC50: 3 nM		99%+
Barasertib-HQPA		++++ Aurora B, IC50: 0.37 nM			99%+
Hesperadin		+ Aurora B (human), IC50: 250 nM			98%
GSK-1070916		++++ Aurora B-INCENP, IC50: 3.5 nM	+++ Aurora C-INCENP, IC50: 6.5 nM	Tie-2,SIK	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。

产品名称	AMPK ↓ ↑	纯度
WZ4003	++++ NUAK1, IC50: 20 nM NUAK2, IC50: 100 nM	98+%
Dorsomorphin	++ AMPK, Ki: 109 nM	99%
HTH-01-015	+++ NUAK1 , IC50: 100 nM	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。

产品名称	NF-κB ↓ ↑	其他靶点	纯度
PDTC ammonium	✔		98%
QNZ	++++ NF-κB, IC50: 11 nM		99%+
Sodium 4-Aminosalicylate Dihydrate	✔		98%
Sodium Salicylate	✔		95%
Parthenolide	✔	p53	97% HPLC
JSH-23	+ NF-κB, IC50: 7.1 μM		98%
Phenethyl caffeate	✔		98%
Andrographolide	✔		98+%
Curcumin	✔	HDAC,Nrf2	98%
SC75741	+++ NF-κB, EC50: 200 nM		99%+
CBL0137 HCl	++ NF-κB, EC50: 0.47 μM	p53	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。

产品名称	VEGFR1 ↓ ↑	VEGFR2 ↓ ↑	VEGFR3 ↓ ↑	其他靶点	纯度
Motesanib Diphosphate	++++ VEGFR1, IC50: 2 nM	++++ VEGFR2, IC50: 3 nM VEGFR2/Flk1, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	PDGFR,RET	99% (HPLC)
Tivozanib	++ VEGFR1, IC50: 30 nM	+++ VEGFR2, IC50: 6.5 nM	++ VEGFR3, IC50: 15 nM		99%+
Brivanib	+ VEGFR1, IC50: 380 nM	++ VEGFR2, IC50: 25 nM Flk1, IC50: 25 nM			99%+
Regorafenib	+++ VEGFR1, IC50: 13 nM	+++ VEGFR2, IC50: 4.2 nM	+ VEGFR3, IC50: 46 nM	RET	98%
Pazopanib	+++ VEGFR1, IC50: 10 nM	++ VEGFR2, IC50: 30 nM	+ VEGFR3, IC50: 47 nM	PDGFR,FGFR,c-Kit	99%
Sitravatinib	+++ VEGFR1 (FLT1), IC50: 6 nM	+++ VEGFR2 (KDR), IC50: 5 nM	++++ VEGFR3 (FLT4), IC50: 2 nM		99%+
Foretinib	+++ VEGFR1/FLT1, IC50: 6.8 nM	++++ KDR, IC50: 0.86 nM	++++ VEGFR3/FLT4, IC50: 2.8 nM	Tie-2	99%+
MGCD-265 analog	++++ VEGFR1, IC50: 3 nM	++++ VEGFR2, IC50: 3 nM	++++ VEGFR3, IC50: 4 nM	Tie-2	99%+
Lactate	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	85%
AEE788	+ FLT1, IC50: 59 nM	+ KDR, IC50: 77 nM		EGFR	98+%
Linifanib	++++ VEGFR1/FLT1, IC50: 3 nM	++++ VEGFR2/KDR, IC50: 4 nM	+ VEGFR3/FLT4, IC50: 190 nM	FLT3	99%+
Vatalanib 2HCl	+ VEGFR1/FLT1, IC50: 77 nM	++ VEGFR2/Flk1, IC50: 270 nM VEGFR2/KDR, IC50: 37 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Fms,c-Kit	99%+
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/Flk1, IC50: 0.18 nM VEGFR2/KDR, IC50: 0.2 nM			98%
Dovitinib	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	99%+
ZM 306416	+ VEGFR1, IC50: 0.33 μM			Src	99%+
KRN-633	+ VEGFR1, IC50: 170 nM	+ VEGFR2, IC50: 160 nM	+ VEGFR3, IC50: 125 nM	BTK,c-Kit	98%
OSI-930	+++ FLT1, IC50: 8 nM	+++ KDR, IC50: 9 nM			99%+
Lenvatinib	++ VEGFR1/FLT1, IC50: 22 nM	++++ VEGFR2/KDR, IC50: 4.0 nM	+++ VEGFR3/FLT4, IC50: 5.2 nM		98%
NVP-BAW2881	+ hVEGFR1, IC50: 820 nM	+++ hVEGFR2, IC50: 9 nM mVEGF2, IC50: 165 nM	+ hVEGFR3, IC50: 420 nM		99%
Cediranib	+++ VEGFR1/FLT1, IC50: 5 nM	++++ VEGFR2/KDR, IC50: 0.5 nM		c-Kit	99%+
Nintedanib	++ VEGFR1, IC50: 34 nM	+++ VEGFR2, IC50: 13 nM	+++ VEGFR3, IC50: 13 nM	FLT3	99+%
BMS-794833		++ VEGFR2, IC50: 15 nM			99%+
SKLB1002		++ VEGFR2, IC50: 32 nM			99%
Cabozantinib S-malate		++++ VEGFR2/KDR, IC50: 0.035 nM			99+%
Ki8751		++++ VEGFR2, IC50: 0.9 nM		c-Kit	99%
SU 5402		++ VEGFR2, IC50: 20 nM			98%
Rivoceranib Mesylate		++++ VEGFR2, IC50: 1 nM		RET	98+%
Ponatinib		++++ VEGFR2, IC50: 1.5 nM			98%
LY2874455		+++ VEGFR2, IC50: 7 nM			99%+
ZM323881 HCl		++++ VEGFR2, IC50: <2 nM			98%
AZD2932		+++ VEGFR-2, IC50: 8 nM		c-Kit	99%
Cabozantinib		++++ VEGFR2/KDR, IC50: 0.035 nM			98%
Sorafenib		++ VEGFR2, IC50: 90 nM VEGFR2/Flk1, IC50: 90 nM			99%
CYC-116		++ VEGFR2, Ki: 44 nM		FLT3	99%+
Golvatinib		++ VEGFR2, IC50: 16 nM			99%+
Sunitinib		+ VEGFR2 , IC50: 80 nM		FLT3	98%
RAF265		++ VEGFR2, EC50: 30 nM			99%+
PD173074					99%+
BFH772		++++ VEGFR2, IC50: 3 nM			98%
Semaxinib		+ VEGFR2/Flk1, IC50: 1.23 μM			98%
Vandetanib		++ VEGFR2, IC50: 40 nM	+ VEGFR3, IC50: 110 nM	EGFR	99%
SAR131675			++ VEGFR3, IC50: 23 nM		99%+
ENMD-2076		+ VEGFR2/KDR, IC50: 58.2 nM	++ VEGFR3/FLT4, IC50: 15.9 nM	FLT3,RET	98%
Telatinib		+++ VEGFR2, IC50: 6 nM	++++ VEGFR3, IC50: 4 nM	c-Kit	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。

产品名称	c-Kit ↓ ↑	其他靶点	纯度
Tyrphostin AG1296	+ c-Kit (Swiss 3T3), IC50: 1.8 μM	PDGFR	99%+
Masitinib	+ Kit, IC50: 200 nM		99%+
Motesanib Diphosphate	+++ Kit, IC50: 8 nM		99% (HPLC)
Ki8751	++ c-Kit, IC50: 40 nM		99%
Tivozanib	++ c-Kit, IC50: 78 nM		99%+
Pazopanib	+ c-Kit, IC50: 140 nM		99%
Sitravatinib	+++ Kit, IC50: 6 nM		99%+
Pexidartinib	+++ Kit, IC50: 10 nM		99%+
Lactate	++++ c-Kit, IC50: 2 nM	FLT3	85%
Amuvatinib	+++ c-Kit (D816H), IC50: 10 nM		99%+
Imatinib Mesylate	+ c-Kit, IC50: 100 nM	PDGFR	99%
AZD2932	+++ c-Kit, IC50: 9 nM		99%
Axitinib	++++ Kit, IC50: 1.7 nM		98%
Dovitinib	++++ c-Kit, IC50: 2 nM	FLT3	99%+
Sunitinib	✔	FLT3	98%
OSI-930	+ Kit, IC50: 80 nM		99%+
Telatinib	++++ c-Kit, IC50: 1 nM		99%+
Dasatinib monohydrate	++ c-Kit (wt), IC50: 79 nM c-Kit (D816V), IC50: 37 nM	Src	98%
Dasatinib	++ c-Kit (wt), IC50: 79 nM c-Kit (D816V), IC50: 37 nM	Src	98%
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。

产品名称	PDGFR ↓ ↑	PDGFRα ↓ ↑	PDGFRβ ↓ ↑	其他靶点	纯度
Tyrphostin A9	+ PDGFR, IC50: 0.5 μM			EGFR	98%
Tyrphostin AG1296					99%+
Motesanib Diphosphate	++ PDGFR, IC50: 84 nM				99% (HPLC)
Pazopanib	++ PDGFR, IC50: 84 nM				99%
Imatinib	+ PDGFR, IC50: 100 nM			c-Kit	98%
Imatinib Mesylate	+ PDGFR, IC50: 100 nM			c-Kit	99%
Sennoside B	✔				99%+
PP121	++++ PDGFR, IC50: 2 nM			VEGFR,mTOR	99%+
Crenolanib		++++ PDGFRα, Kd: 2.1 nM	++++ PDGFRβ, Kd: 3.2 nM		99%+
Masitinib		+ PDGFRα, IC50: 540 nM	+ PDGFRβ, IC50: 800 nM		99%+
Ki8751		++ PDGFRα, IC50: 67 nM		c-Kit	99%
Tivozanib		++ PDGFRα, IC50: 40 nM	++ PDGFRβ, IC50: 49 nM		99%+
Ponatinib		++++ PDGFRα, IC50: 1.1 nM			98%
Amuvatinib		++ PDGFRα (V561D), IC50: 40 nM			99%+
Axitinib		+++ PDGFRα, IC50: 5.0 nM	++++ PDGFRβ, IC50: 1.6 nM		98%
CP-673451		+++ PDGFRα, IC50: 10 nM	++++ PDGFRβ, IC50: 1 nM		99%+
Telatinib		+++ PDGFRα, IC50: 15 nM		c-Kit	99%+
Nintedanib		++ PDGFRα, IC50: 59 nM	++ PDGFRβ, IC50: 65 nM		99+%
Avapritinib		++++ PDGFRα (D842V), IC50: 0.5 nM			99%+
MK-2461			+++ PDGFRβ, IC50: 22 nM		98%+
Lactate			+++ PDGFRβ, IC50: 27 nM	FLT3,c-Kit	85%
Linifanib			++ PDGFRβ, IC50: 66 nM		99%+
AZD2932			+++ PDGFRβ, IC50: 4 nM	c-Kit	99%
Dovitinib			+++ PDGFRβ, IC50: 27 nM	FLT3,c-Kit	99%+
Sorafenib			++ PDGFRβ, IC50: 57 nM mPDGFRβ, IC50: 57 nM		99%
Sunitinib			++++ PDGFRβ , IC50: 2 nM	FLT3	98%
Orantinib			+++ PDGFRβ, Ki: 8 nM		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。

(Z)-Orantinib 生物活性

描述

Vascular endothelial growth factor (VEGF), fibroblast growth factor (FGF), and platelet-derived growth factor (PDGF) and their cognate receptor tyrosine kinases are strongly implicated in angiogenesis associated with solid tumors. SU6668 is a novel inhibitor of these receptors. SU6668 is a competitive inhibitor, with regard to ATP, of Flk-1 trans-phosphorylation (K_i = 2.1 μM), FGFR1 trans-phosphorylation (K_i = 1.2 μM), and PDGFR autophosphorylation (K_i = 0.008 μM). HUVECs stimulated by VEGF exhibit an increase in tyrosine phosphorylation of KDR. Treatment of cells with SU6668 inhibited this increase in a dose-dependent manner. SU6668 also inhibited PDGF-stimulated PDGFRβ tyrosine phosphorylation in NIH-3T3 cells overexpressing PDGFRβ at a minimum concentration of 0.03–0.1 μM. SU6668 inhibited acidic FGF-induced phosphorylation of the FGFR1 substrate 2 (FRS-2) at concentrations of 10 μM and higher. SU6668 inhibited VEGF-driven mitogenesis of HUVECs in a dose-dependent manner with a mean IC₅₀ of 0.34 ± 0.05 μM. p.o. administered SU6668 induced dose-dependent inhibition of A431 tumor growth in the s.c. xenograft model in athymic mice. SU6668 was also efficacious when administered i.p. or p.o. in additional xenograft models, including A375, Colo205, H460, Calu-6, C6, SF763T, and SKOV3TP5 cells. These in vivo data demonstrated that SU6668 readily induced >75% growth inhibition against a broad range of tumor types^[3].

作用机制

In both FGFR1 and PDGFR, the oxindole core structure of SU6668 forms hydrogen bonds with the receptor backbone at the hinge region^[3].

(Z)-Orantinib 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00784290	Hepatocellular Carcinoma	Phase 1 Phase 2	Completed	-	Japan ... 展开 >> Chiba University Hospital Inohana Chuo-ku Chiba, Chiba, Japan, 260-8670 收起 <<
NCT00024063	Breast Cancer ... 展开 >> Colorectal Cancer Gastric Cancer Kidney Cancer Lung Cancer Multiple Myeloma and Plasma Cell Neoplasm Pancreatic Cancer Prostate Cancer 收起 <<	Phase 1	Unknown	-	-
NCT01465464	Hepatocellular Carcinoma	Phase 3	Terminated	-	Japan ... 展开 >> Local Institution Osaka-sayama, Osaka, Japan, 589-8511 Local Institution Chuo-ku, Tokyo, Japan, 104-0045 Local Institution Chiba, Japan, 260-8677 Korea, Republic of Local Institution Goyang-si, Gyeonggi-do, Korea, Republic of, 410-769 Local Institution JongNo-Gu, Seoul, Korea, Republic of, 110-744 Taiwan Local Institution Zhongzheng Dist., Taipei, Taiwan, 100 收起 <<

(Z)-Orantinib 参考文献

[1]Qian B, Yao Y, et al. SU6668 modulates prostate cancer progression by downregulating MTDH/AKT signaling pathway. Int J Oncol. 2017 May;50(5):1601-1611.

[2]Ge Y, Ding Y, et al. Effect of angiogenesis inhibitor SU6668 in combination with 5-Fu on liver metastasis from transplantation tumors of human colorectal cancer in nude mice. Int J Clin Exp Med. 2014 Oct 15;7(10):3578-82.

[3]SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors

(Z)-Orantinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.22mL

0.64mL

0.32mL

16.11mL

3.22mL

1.61mL

32.22mL

6.44mL

3.22mL

(Z)-Orantinib 技术信息

CAS号	210644-62-5
分子式	C₁₈H₁₈N₂O₃
分子量	310.35
SMILES Code	O=C(O)CCC1=C(C)NC(/C=C2C(NC3=C\2C=CC=C3)=O)=C1C
MDL No.	MFCD09743433

别名	SU6668; (Z)-TSU-68; (Z)-SU6668
运输	蓝冰
InChI Key	NHFDRBXTEDBWCZ-ZROIWOOFSA-N
Pubchem ID	5329099

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, room temperature

溶解方案

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

(Z)-Orantinib {[allProObj[0].p_purity_real_show]}

(Z)-Orantinib 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

(Z)-Orantinib 质控信息

(Z)-Orantinib 生物活性

(Z)-Orantinib 临床研究

(Z)-Orantinib 参考文献

(Z)-Orantinib 实验方案

(Z)-Orantinib 技术信息

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