Dasatinib monohydrate | BMS-354825 monohydrate | Src/Bcr-Abl Inhibitor

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达沙替尼（一水合物） /Dasatinib monohydrate {[allProObj[0].p_purity_real_show]}

货号：A210354 同义名： BMS-354825 monohydrate

Dasatinib monohydrate（BMS-354825）是一种高效的ATP竞争性口服活性双重Src/Bcr-Abl抑制剂，具有显著的抗肿瘤活性。其对Src和Bcr-Abl的Ki值分别为16 pM和30 pM，对Bcr-Abl和Src的IC50值分别为<1.0 nM和0.5 nM。达沙替尼一水合物还诱导细胞凋亡和自噬。

Dasatinib monohydrate 化学结构
CAS号：863127-77-9

Dasatinib monohydrate 3D分子结构
CAS号：863127-77-9

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Dasatinib monohydrate 纯度/质量文件产品仅供科研

货号：A210354 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

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

c-Kit 亚型比较
转化生长因子-β 亚型比较
Bcr-Abl 亚型比较
Src 亚型比较

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		98%
Ki8751	++ c-Kit, IC50: 40 nM		98+%
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		98%
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	ALK1 ↓ ↑	ALK2 ↓ ↑	ALK3 ↓ ↑	ALK4 ↓ ↑	ALK6 ↓ ↑	Smad3 ↓ ↑	TGF-β ↓ ↑	TGFβRI/ALK5 ↓ ↑	TGFβRII ↓ ↑	纯度
LDN193189	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%+
LDN-212854	++++ ALK1, IC50: 2.4 nM	++++ ALK2, IC50: 1.3 nM	+ ALK3, IC50: 85.8 nM	+ ALK4, IC50: 2133 nM				+ ALK5, IC50: 9276 nM		99%+
ML347	++ ALK1, IC50: 46 nM	++ ALK2, IC50: 32 nM								98%
K02288	++++ ALK1, IC50: 1.8 nM	++++ ALK2, IC50: 1.1 nM	++ ALK3, IC50: 34.4 nM		+++ ALK6, IC50: 6.4 nM					99%+
LDN-193189 dihydrochloride	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%
LDN-214117		++ ALK2, IC50: 24 nM								98%
DMH-1		+ ALK2, IC50: 107.9 nM								99%+
SB-505124				+ ALK4, IC50: 129 nM				++ ALK5, IC50: 47 nM		99%+
Vactosertib				+++ ALK4, IC50: 13 nM				+++ ALK5, IC50: 11 nM		99%+
Alantolactone						✔				98%
SIS3						✔				97%
Pirfenidone							✔			98%
Hesperetin							✔			97%
RepSox								++++ TGFβR1(ALK5), IC50: 4 nM		98%
GW788388								+++ ALK5, IC50: 18 nM		98%
LY364947								++ TGFβRI, IC50: 59 nM	+ TGFβRII, IC50: 0.4 μM	98%
SD-208								++ TGF-βRI (ALK5), IC50: 48 nM		98%
SB-525334								+++ TGFβR1(ALK5), IC50: 14.3 nM		99%+
LY2109761								++ TβRI, Ki: 38 nM	+ TβRII, Ki: 300 nM	99%+
Galunisertib								++ TβRI, IC50: 56 nM		98%
SB 431542								+ ALK5, IC50: 94 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	Abl ↓ ↑	Bcr-Abl ↓ ↑	其他靶点	纯度
NVP-BHG 712	+ c-Abl, IC50: 1.667 μM			99%+
KW-2449	+++ Abl (T315I), IC50: 4 nM Abl, IC50: 14 nM		FLT3	99%+
Ponatinib	++++ Abl, IC50: 0.37 nM			98%
AT9283				99%+
Imatinib Mesylate	+ v-Abl, IC50: 600 nM		c-Kit,PDGFR	99%
Danusertib	++ Abl, IC50: 25 nM		RET	99%+
Rebastinib	++++ u-Abl1 (T315I), IC50: 5 nM p-Abl1 (native), IC50: 0.75 nM		Tie-2,FLT3	99%+
PP121	++ Abl, IC50: 18 nM		PDGFR,VEGFR	99%+
GNF-7	+++ E255V, IC50: 122 nM M351T, IC50: 133 nM			99%+
Olverembatinib dimesylate	++++ Abl (G250E), IC50: 0.35 nM Abl, IC50: 0.34 nM			99%
Dasatinib monohydrate	++++ Abl , IC50: 0.6 nM		Src	98%
Dasatinib	++++ Abl, IC50: 0.6 nM		Src	98%
Bafetinib	+++ Abl, IC50: 5.8 nM			98+%
GNF-2		+ Bcr-Abl (K562 cell line), IC50: 273 nM Bcr-Abl (SUP-B15 cell line), IC50: 268 nM		98%+
Degrasyn		+ Bcr-Abl, IC50: 1.8 μM	DUB	98+%
GNF-5		++ Bcr-Abl, IC50: 220 nM		98%
Radotinib		++ BCR-ABL1, IC50: 34 nM		98+%
PD173955			Src	99%+
Nilotinib		++ Bcr-Abl, IC50: <30 nM		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	Fyn ↓ ↑	Lck ↓ ↑	Lyn ↓ ↑	Src ↓ ↑	Yes ↓ ↑	其他靶点	纯度
Saracatinib	++ Fyn, IC50: 10 nM	++++ LCK, IC50: <4 nM	+++ Lyn, IC50: 5 nM	++++ c-Src, IC50: 2.7 nM			99%+
SU6656	+ Fyn, IC50: 170 nM		+ Lyn, IC50: 130 nM	+ Src, IC50: 280 nM	++ YES, IC50: 20 nM		98%
PP1	+++ Fyn, IC50: 6 nM	+++ LCK, IC50: 5 nM				EGFR	99%+
PP2	+++ Fyn, IC50: 5 nM	++++ LCK, IC50: 4 nM					98%
WH-4-023		++++ Lck, IC50: 2 nM		+++ Src, IC50: 6 nM			99%+
NVP-BHG 712				+ c-Src, IC50: 1.266 μM			99%+
CCT196969		++ LCK, IC50: 0.02 μM		+ Src, IC50: 0.03 μM			98%
MNS				+ Src, IC50: 29.3 μM		p97,Syk	98%
Tirbanibulin				++ Src (HuH7), GI50: 13 nM Src (Hep 3B), GI50: 26 nM			99%+
PP121				++ Src, IC50: 14 nM		PDGFR,VEGFR	99%+
Bosutinib				++++ Src, IC50: 1.2 nM			99%
Dasatinib monohydrate				++++ Src, IC50: 0.8 nM			98%
Quercetin				✔		Sirtuin,PKC	97%
Dasatinib				++++ Src, IC50: 0.8 nM			98%
Repotrectinib				+++ Src, IC50: 5.3 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。

Dasatinib monohydrate 生物活性

靶点

c-Kit

c-Kit (wt), IC50:79 nM

c-Kit (D816V), IC50:37 nM
Src

Src, IC50:0.8 nM
Abl

Abl , IC50:0.6 nM

描述

Dasatinib monohydrate, also known as BMS-354825 monohydrate, is an orally active, ATP-competitive dual Src/Bcr-Abl inhibitor with potent antitumor properties. It has Ki values of 16 pM for Src and 30 pM for Bcr-Abl. The IC50 values for inhibiting Bcr-Abl and Src are less than 1.0 nM and 0.5 nM, respectively. Dasatinib monohydrate exhibits significant activity against a range of targets including Bcr-Abl, Src, Lck, Yes, c-Kit, PDGFRβ, p38, Her1, Her2, FGFR-1, and MEK, with IC50 values of less than 1.0, 0.50, 0.40, 0.50, 5.0, 28, 100, 180, 720, 880, and 1700 nM, respectively. It shows antiproliferative effects on K562 chronic myelogenous leukemia (CML), PC3 human prostate cancer, MDA-MB-231 human breast cancer, and WiDr human colon cancer cell lines, with IC50 values of less than 1.0 nM, 9.4 nM, 12 nM, and 52 nM, respectively. Dasatinib monohydrate also induces apoptosis and autophagy in cells^[1].

Dasatinib monohydrate 动物研究

Animal study

The pharmacokinetic profile of Dasatinib monohydrate at 10 mg/kg is suitable for further in vivo efficacy studies, displaying favorable half-lives for both intravenous and oral administration, at 3.3 and 3.1 hours, respectively. The oral bioavailability observed in this study is 27%. At doses of 5 mg/kg and 50 mg/kg, administered once daily for 10 days with a 5 days on and 2 days off schedule, Dasatinib monohydrate demonstrates effective antitumor activity and high safety in a K562 CML xenograft model, resulting in complete tumor regression and low toxicity at multiple dose levels^[1].

Dasatinib monohydrate 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
NCT02883049	B Acute Lymphoblastic Leukemia... 展开 >> Central Nervous System Leukemia Ph-Like Acute Lymphoblastic Leukemia Testicular Leukemia Untreated Adult Acute Lymphoblastic Leukemia Untreated Childhood Acute Lymphoblastic Leukemia 收起 <<	Phase 3	Recruiting	-	-
NCT00390793	Acute Lymphoblastic Leukemia ... 展开 >> BCR-ABL1 Fusion Protein Expression Blast Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive Philadelphia Chromosome Positive Recurrent Acute Lymphoblastic Leukemia t(9;22) 收起 <<	Phase 2	Active, not recruiting	August 31, 2020	United States, Texas ... 展开 >> M D Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT02143414	Acute Lymphoblastic Leukemia ... 展开 >> B Acute Lymphoblastic Leukemia B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1 B Acute Lymphoblastic Leukemia, Philadelphia Chromosome Negative Philadelphia Chromosome Positive Recurrent Adult Acute Lymphoblastic Leukemia Refractory Adult Acute Lymphoblastic Leukemia Untreated Adult Acute Lymphoblastic Leukemia 收起 <<	Phase 2	Recruiting	-	-

Dasatinib monohydrate 参考文献

[1]Lombardo LJ, et al. Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J Med Chem. 2004 Dec 30;47(27):6658-61.

Dasatinib monohydrate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.88mL

1.98mL

0.99mL

19.76mL

3.95mL

1.98mL

Dasatinib monohydrate 技术信息

CAS号	863127-77-9
分子式	C₂₂H₂₈ClN₇O₃S
分子量	506.021

别名	BMS-354825 monohydrate
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 105 mg/mL(207.5 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

动物实验配方

2% DMSO+30% PEG 300+dd water 5 mg/mL

达沙替尼（一水合物） /Dasatinib monohydrate {[allProObj[0].p_purity_real_show]}

Dasatinib monohydrate 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Dasatinib monohydrate 质控信息

Dasatinib monohydrate 生物活性

Dasatinib monohydrate 动物研究

Dasatinib monohydrate 临床研究

Dasatinib monohydrate 参考文献

Dasatinib monohydrate 实验方案

Dasatinib monohydrate 技术信息

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c-Kit	c-Kit (wt), IC50:79 nM c-Kit (D816V), IC50:37 nM
Src	Src, IC50:0.8 nM
Abl	Abl , IC50:0.6 nM

达沙替尼（一水合物） /Dasatinib monohydrate {[allProObj[0].p_purity_real_show]}

Dasatinib monohydrate 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Dasatinib monohydrate 质控信息

Dasatinib monohydrate 生物活性

Dasatinib monohydrate 动物研究

Dasatinib monohydrate 临床研究

Dasatinib monohydrate 参考文献

Dasatinib monohydrate 实验方案

Dasatinib monohydrate 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

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Dasatinib monohydrate 纯度/质量文件产品仅供科研