Corosolic acid | Colosolic acid | Autophagy Inducer | AmBeed-信号通路专用抑制剂

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产品名称	EGFR/ErbB1 ↓ ↑	ErbB3 ↓ ↑	ErbB4 ↓ ↑	HER2/ErbB2 ↓ ↑	mutant EGFR ↓ ↑	其他靶点	纯度
WZ-3146	++++ EGFR (E746_A750), IC50: 2 nM EGFR (E746_A750/T790M), IC50: 14 nM						99%+
Daphnetin	+ EGFR, IC50: 7.67 μM					PKA,PKC	95%
Lifirafenib	++ EGFR, IC50: 29 nM				+ EGFR(T790M/L858R), IC50: 495 nM		98%
PD168393	++++ EGFR, IC50: 0.70 nM						99%+
Nazartinib	++ mutant EGFR, Ki: 0.031 μM				++ mutant EGFR, Ki: 0.031 μM		98%
Norcantharidin	✔						98%
CL-387785	++++ EGFR, IC50: 370 pM						98%
WHI-P154	+++ EGFR, IC50: 4 nM					VEGFR,Src	98%
Tyrphostin A9	+ EGFR, IC50: 460 μM					PDGFR	98%
AG 555	+ EGFR, IC50: 0.7 μM						98%
AG 494	+ EGFR, IC50: 1.2 μM						99%+
AG-556	+ EGFR, IC50: 5 μM						98%
RG13022	+ EGFR, IC50: 4 μM						99%+
Tyrphostin RG 14620	✔						99%+
Vandetanib	+ EGFR, IC50: 500 nM						99%
CNX-2006	++ mutant EGFR, IC50: <20 nM				++ mutant EGFR, IC50: <20 nM		99%
AZD3759	++++ EGFR (L858R), IC50: 0.2 nM EGFR (WT), IC50: 0.3 nM						98%
Erlotinib	++++ EGFR, IC50: 2 nM						95%
Saracatinib	+++ EGFR, IC50: 5 nM EGFR (L861Q), IC50: 4 nM						99%+
AG1557	✔						99%
Rociletinib	++ EGFR (L858R/T790M), Ki: 21.5 nM EGFR (wt), Ki: 303.3 nM						98%
AG490	+ EGFR, IC50: 0.1 μM						98%
Cetuximab	++++ EGFR, Kd: 0.39 nM						95%
Osimertinib	++ WT EGFR, IC50: 12.92 nM L858R/T790M EGFR, IC50: 11.44 nM						98%
Osimertinib mesylate	✔						98% (Content MsOH 15.2-18.2%)
Chrysophanol	✔					mTOR	98%
PD153035	++++ EGFR, Ki: 5.2 pM						99%+
Olmutinib	✔					BTK	99%+
WZ4002	++++ EGFR (L858R), IC50: 2 nM EGFR (L858R/T790M), IC50: 8 nM						99%+
Icotinib	+++ EGFR, IC50: 5 nM						99%
Desmethyl Erlotinib HCl	++++ EGFR, IC50: 2 nM						98%
Cyasterone	✔						99%+
PP 3	+ EGFR tyrosine kinase, IC50: 2.7 μM						98%
WZ8040	✔						99%+
(-)-Epigallocatechin Gallate	✔						99%
AG 18	+ EGFR, IC50: 35 μM						99%+
O-Desmethyl gefitinib	++ EGFR, IC50: 36 nM						99%
Falnidamol	✔						99%+
AZ-5104	++++ EGFR (L858R), IC50: 6 nM EGFR (L861Q) , IC50: <1 nM		+++ ErbB4, IC50: 7 nM			BRK	99%+
Butein	✔						95%
Genistein	✔						98%
SU5214	+ EGFR, IC50: 36.7 μM						99%+
Naquotinib	✔						99%+
Gefitinib	++ EGFR, IC50: 15.5 nM				+ EGFR (858R/T790M), IC50: 823.3 nM		98%
Theliatinib	+++ WT EGFR, IC50: 3 nM				++ EGFR T790M/L858R, IC50: 22 nM		99%
Lazertinib	++++ WT EGFR, IC50: 76 nM L858R/T790M EGFR, IC50: 2 nM				++++ Del19/T790M, IC50: 1.7 nM		99%+
Gefitinib-based PROTAC 3	++ EGFR, DC50: 22.3 nM						99%+
MTX-211	✔					PI3K	98%
(E)-AG 99	✔						99%+
Licochalcone D	✔					Caspase,PARP	99%
Zipalertinib	+++ EGFR WT, IC50: 8 nM EGFR (L861Q), IC50: 4.1 nM		+++ HER4, IC50: 4 nM		++++ EGFR(d746-750), IC50: 1.4 nM EGFR L858R, IC50: 2 nM		97%
JND3229	+++ EGFR WT, IC50: 6.8 nM				++ EGFR L858R/T790M, IC50: 30.5 nM		99%+
Firmonertinib mesylate	✔						99%+
Tyrphostin AG30	✔						99%+
EGFR-IN-12	++ EGFR, IC50: 21 nM						99%+
Mobocertinib	✔						98%
(Rac)-JBJ-04-125-02	✔						95%
(S)-Sunvozertinib	✔						99%
BLU-945	✔						95%
Poziotinib	+++ HER1, IC50: 3.2 nM		++ HER4, IC50: 23.5 nM	+++ HER2, IC50: 5.3 nM			98%
TAK-285	++ EGFR/HER1, IC50: 23 nM		+ HER4, IC50: 260 nM	++ HER2, IC50: 17 nM			99%+
ARRY-380 analog				✔			99%
Canertinib	++++ EGFR, IC50: 1.5 nM			+++ ErbB2, IC50: 9.0 nM			99%+
Dacomitinib	+++ EGFR, IC50: 6.0 nM		+ ErbB4, IC50: 73.7 nM	+ ErbB2, IC50: 45.7 nM			98%
EGFR/ErbB-2/ErbB-4 inhibitor-2			+ ErbB4, IC50: 1.91 μM	+ ErbB2, IC50: 0.08 μM			99%+
(E/Z)-CP-724714				++ HER2/ErbB2, IC50: 10 nM			95%
Lapatinib	++ EGFR, IC50: 10.8 nM		+ ErbB4, IC50: 367 nM	+++ ErbB2, IC50: 9.2 nM			98%
AEE788	++++ EGFR, IC50: 2 nM		+ HER4/ErbB4, IC50: 160 nM	+++ HER2/ErbB2, IC50: 6 nM		c-Fms/CSF1R	98+%
AV-412 free base	++++ EGFR, IC50: 0.75 nM			++ ErbB2, IC50: 19 nM	++++ EGFR^L858R/T790M, IC50: 0.51 nM EGFR^T790M, IC50: 0.79 nM		98+%
Neratinib	+ EGFR, IC50: 92 nM			+ HER2, IC50: 59 nM		Src	98%
BMS-599626	++ HER1, IC50: 20 nM		+ HER4, IC50: 190 nM	++ HER2, IC50: 30 nM			98%
Tucatinib				+++ ErbB2, IC50: 8 nM			98%
Allitinib	++++ EGFR, IC50: 0.5 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Pelitinib	+ EGFR, IC50: 38.5 nM			+ ErbB2, IC50: 1.255 μM		Src,Raf	99%+
Sapitinib	+++ EGFR, IC50: 4 nM	+++ ErbB3, IC50: 4 nM		+++ ErbB2, IC50: 3 nM			99%+
CUDC-101	+++ EGFR, IC50: 2.4 nM			++ HER2, IC50: 15.7 nM		HDAC	99%+
Varlitinib	+++ ErbB1, IC50: 7 nM			++++ ErbB2, IC50: 2 nM			99%+
Afatinib dimaleate	++++ EGFR (L858R/T790M), IC50: 0.4 nM EGFR (wt), IC50: 0.5 nM			++ HER2, IC50: 14 nM			98%
Canertinib 2HCl	+++ EGFR, IC50: 7.4 nM			+++ ErbB2, IC50: 9 nM			99%
Allitinib tosylate	++++ EGFR, IC50: 0.5 nM EGFR (T790M/L858R), IC50: 12 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Tyrphostin AG 528	+ EGFR, IC50: 4.9 μM			+ HER2, IC50: 2.1 μM			97%
Afatinib	++++ EGFR (L858R), IC50: 10 nM EGFR (wt), IC50: 0.5 nM		++++ ErbB4, IC50: 1 nM	++ HER2, IC50: 14 nM			99%
Pyrotinib dimaleate	++ EGFR, IC50: 0.013 μM			++ HER2, IC50: 0.038 μM			98%
Epertinib HCl	++++ EGFR, IC50: 1.48 nM		+++ HER4, IC50: 2.49 nM	+++ HER2, IC50: 7.15 nM			99%
Tuxobertinib	++++ EGFR, Kd: 0.2 nM			++++ HER2, Kd: 0.76 nM			99%
ALK-IN-1					++ EGFR(C797S/del19), IC50: 138.6 nM EGFR(del19), IC50: 36.8 nM	ALK	99%
Brigatinib					+ EGFR(del19), IC50: 39.9 nM EGFR(C797S/T790M/del19), IC50: 67.2 nM	ALK,FLT3	98%
Avitinib					++++ EGFR L858R/T790M, IC50: 0.18 nM	BTK	99%+
EAI045					✔		97%
Almonertinib					✔		99%
BI-4020					++++ EGFR^{del19 T790M C797S}, IC50: 0.2 nM		99%+
EGFR-IN-7					++++ EGFR^L858R/T790M, IC50: 0.19 nM EGFR^{d746-750/T790M/C797S}, IC50: 0.26 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	MMP ↓ ↑	纯度
Marimastat	+++ MMP-7, IC50: 16 nM MMP-14, IC50: 3 nM	98%
Ilomastat	++++ MMP-26, Ki: 0.36 nM MMP-2, Ki: 0.1 nM	99%+
SB-3CT	+ MMP-9, Ki: 600 nM MMP-2, Ki: 13.9 nM	99%+
Doxycycline	✔	95%
NSC 405020	✔	98%
Batimastat	+++ MMP-7, IC50: 4 nM MMP-1, IC50: 3 nM	99%+
Nobiletin	✔	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	Autophagy ↓ ↑	其他靶点	纯度
SBI-0206965	+++ ULK2, IC50: 711 nM ULK1, IC50: 108 nM		99%
Hydroxychloroquine sulfate	✔		99%
Valproic acid sodium	✔	HDAC	97%
PFK-015	++ PFKFB3, IC50: 207 nM		99%+
MRT68921 HCl	++++ ULK2, IC50: 1.1 nM ULK1, IC50: 2.9 nM		99%+
ROC-325	✔		99%+
Autophinib	+++ Autophagy, IC50: 40 nM		99%
Lys05	✔		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。

Cell Line H9C2 cells U373 glioblastoma cells THP-1 macrophages Human monocyte-derived macrophages (HMDM) Rat chondrocytes Neonatal rat ventricular myocytes (NRVMs) HL-7702 SK-Hep1 SMMC-7721 Bel-7402 Bel-7404 DU145 cells PC-3 cells	Concentration	Treated Time	Description	References
H9C2 cells	1, 5, 10 µM	24 h	To investigate the protective effect of CRA on hypoxia-induced H9C2 cells, results showed that CRA inhibited the expression of Nox2 and Nox4, increased HO-1 expression, reduced ROS production and apoptosis.	Int J Mol Med. 2020 May;45(5):1425-1435
U373 glioblastoma cells	20-100 μM	24 h	Inhibited cell proliferation by suppressing constitutive activation of STAT3 and NF-κB	Cancer Sci. 2011 Jan;102(1):206-11
THP-1 macrophages	30 μM	24 h	Suppressed TCS-induced IL-10 secretion and enhanced IL-6 and IL-12 secretion, indicating Corosolic acid shifts M2 polarization to M1 polarization	Cancer Sci. 2011 Jan;102(1):206-11
Human monocyte-derived macrophages (HMDM)	30 μM	24 h	Inhibited IL-10-induced CD163 expression, indicating Corosolic acid suppresses M2 polarization of macrophages	Cancer Sci. 2011 Jan;102(1):206-11
Rat chondrocytes	0, 2.5, 5, 10 μM	24 h	To evaluate the effect of corosolic acid on ECM metabolism of chondrocytes. Results showed that CRA reversed the IL-1β-induced degradation of aggrecan and type II collagen and the high expression of MMP13 and ADAMTS5.	Drug Des Devel Ther. 2022 Aug 6;16:2627-2637
Neonatal rat ventricular myocytes (NRVMs)	10 μg/mL	24 h	To study the protective effect of CA on mitochondrial structure and function after H/R injury, results showed CA reduced mitochondrial swelling and vacuolation, and restored mitochondrial membrane potential.	iScience. 2024 Jul 8;27(8):110448
HL-7702	40 μM	24 h	inhibited cell proliferation	Cell Death Dis. 2021 Sep 29;12(10):889
SK-Hep1	40 μM	24 h	inhibited cell proliferation	Cell Death Dis. 2021 Sep 29;12(10):889
SMMC-7721	40 μM	24 h	inhibited cell proliferation	Cell Death Dis. 2021 Sep 29;12(10):889
Bel-7402	40 μM	24 h	inhibited cell proliferation and promoted apoptosis	Cell Death Dis. 2021 Sep 29;12(10):889
Bel-7404	40 μM	24 h	inhibited cell proliferation and promoted apoptosis	Cell Death Dis. 2021 Sep 29;12(10):889
DU145 cells	5, 10, 15 μM	24 h	CA inhibited DU145 cell growth and induced apoptosis via activation of IRE-1/JNK and PERK/CHOP signaling pathways.	J Exp Clin Cancer Res. 2018 Sep 3;37(1):210
PC-3 cells	5, 10, 15 μM	24 h	CA inhibited PC-3 cell growth and induced apoptosis via activation of IRE-1/JNK and PERK/CHOP signaling pathways.	J Exp Clin Cancer Res. 2018 Sep 3;37(1):210

Species Sprague-Dawley (SD) rats Wistar rats Sprague-Dawley rats BALB/c nude mice Nude mice	Animal Model Orthotopic liver cancer model with ALPPS procedure Surgically induced OA model (ACLT) Myocardial ischemia/reperfusion injury model Xenograft mouse model PC-3 xenograft model	Administration	Dosage	Frequency	Description	References
Sprague-Dawley (SD) rats	Orthotopic liver cancer model with ALPPS procedure	Intraperitoneal injection	20 mg/kg	Every two days for 12 days	Corosolic acid inhibits tumour growth without compromising ALPPS-induced liver regeneration. This result may be attributed to the CA-induced downregulation of PD-1 and TGF-β expression and the increased CD8+ lymphocyte infiltration in tumour tissue associated with the suppression of M2 macrophage polarisation.	Ann Med. 2022 Dec;54(1):1188-1201
Wistar rats	Surgically induced OA model (ACLT)	Gavage	20 mg/kg	Once daily for 8 weeks	To evaluate the effect of corosolic acid on OA progression. Results showed that CRA reduced pathological changes such as cartilage erosion, ECM loss, and superficial cartilage destruction, lowered OARSI scores, upregulated COL2A1 and LC3B expression, and downregulated MMP13 expression.	Drug Des Devel Ther. 2022 Aug 6;16:2627-2637
Sprague-Dawley rats	Myocardial ischemia/reperfusion injury model	Intraperitoneal injection	10 mg/kg	Once daily for 14 days	To evaluate the protective effect of CA on myocardial I/R injury, results showed CA significantly improved cardiac function, reduced infarct area, and alleviated mitochondrial damage.	iScience. 2024 Jul 8;27(8):110448
BALB/c nude mice	Xenograft mouse model	Intratumoral injection	10 mg/kg	Daily for 20 days	Inhibited tumor growth	Cell Death Dis. 2021 Sep 29;12(10):889
Nude mice	PC-3 xenograft model	Intraperitoneal injection	10 and 20 mg/kg	Every 2 days for 14 days	CA significantly inhibited the growth of PC-3 xenograft tumors by activating ER stress-dependent apoptotic signaling pathways.	J Exp Clin Cancer Res. 2018 Sep 3;37(1):210

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03388762	Prediabetic State	Not Applicable	Recruiting	September 2019	United States, Maryland ... 展开 >> University of Maryland Center for Diabetes and Endocrinology Recruiting Baltimore, Maryland, United States, 21201 Contact: Kashif Munir, MD 443-682-6800 kmunir@medicine.umaryland.edu University of Maryland Family Medicine Associates Recruiting Baltimore, Maryland, United States, 21201 Contact: Mary Bahr-Robertson 410-706-6155 mbahr@som.umaryland.edu University of Maryland School of Medicine, Department of Family and Community Medicine, East Hall Not yet recruiting Baltimore, Maryland, United States, 21201 Contact: Mary Bahr-Robertson 410-706-6155 mbahr@som.umaryland.edu United States, Ohio Alliance Integrative Medicine Recruiting Cincinnati, Ohio, United States, 45236 Contact: Lisa Gallagher, ND 513-791-5521 lisa.gallagher@myhealingpartner.com 收起 <<

CAS号	4547-24-4
分子式	C₃₀H₄₈O₄
分子量	472.7
SMILES Code	O[C@H]1[C@H](O)C(C)(C)[C@@](CC[C@]2(C)[C@]3([H])CC=C4[C@@]2(C)CC[C@]5(C(O)=O)[C@@]4([H])[C@@H](C)[C@H](C)CC5)([H])[C@]3(C)C1
MDL No.	MFCD06794973

别名	Colosolic acid; Glucosol; 2α-Hydroxyursolic acid; Colosic acid
运输	蓝冰

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