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Dasatinib monohydrate

CAS No.
863127-77-9
Chemical Name:
Dasatinib monohydrate
Synonyms
Sprycel;Dasatinib hydrate;n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide monohydrate;mmbf;Dastinib;CS-295;Dasatinib R;Bms 35482503;Unii-rbz1571X5h;Dasatinib(TINIBS)
CBNumber:
CB4844484
Molecular Formula:
C22H28ClN7O3S
Molecular Weight:
506.02
MDL Number:
MFCD08704581
MOL File:
863127-77-9.mol
MSDS File:
SDS
TDS File:
TDS
Last updated:2026-08-06 18:30:54

Dasatinib monohydrate Properties

Melting point >223° (dec.)
storage temp. Keep in dark place,Sealed in dry,Store in freezer, under -20°C
solubility DMSO (Slightly, Sonicated), Methanol (Slightly, Sonicated)
form Solid
color White to Off-White
Stability Hygroscopic
InChIKey XHXFZZNHDVTMLI-UHFFFAOYSA-N
SMILES N(C1=NC=C(C(=O)NC2C(=CC=CC=2C)Cl)S1)C1N=C(C)N=C(N2CCN(CCO)CC2)C=1.O
CAS DataBase Reference 863127-77-9(CAS DataBase Reference)
FDA UNII RBZ1571X5H
NCI Dictionary of Cancer Terms Sprycel
NCI Drug Dictionary Sprycel

SAFETY

Risk and Safety Statements

Symbol(GHS)  Health Hazard (GHS08)Environment (GHS09)Skull and Crossbones (GHS06)
GHS08,GHS09,GHS06
Signal word  Danger
Hazard statements  H410-H300-H372-H361-H360
Precautionary statements  P264-P270-P301+P310-P321-P330-P405-P501-P260-P264-P270-P314-P501-P273-P391-P501-P201-P202-P281-P308+P313-P405-P501
HS Code  29339900

Dasatinib monohydrate price More Price(54)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Usbiological 270937 Dasatinib Monohydrate ≥99%(HPLC) 863127-77-9 250mg $319 2026-06-03 Buy
Usbiological 270937 Dasatinib Monohydrate ≥99%(HPLC) 863127-77-9 500mg $432 2026-06-03 Buy
Usbiological 270937 Dasatinib Monohydrate ≥99%(HPLC) 863127-77-9 1g $573 2026-06-03 Buy
Usbiological 270937 Dasatinib Monohydrate ≥99%(HPLC) 863127-77-9 5g $1020 2026-06-03 Buy
Biosynth FD10821 Dasatinib monohydrate 863127-77-9 1000mg $280 2026-06-04 Buy
Product number Packaging Price Buy
270937 250mg $319 Buy
270937 500mg $432 Buy
270937 1g $573 Buy
270937 5g $1020 Buy
FD10821 1000mg $280 Buy

Dasatinib monohydrate Chemical Properties, Uses, Production

Description

Dasatinib monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity.

Uses

Dasatinib Monohydrate is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. It is a COVID19-related research product. It is used in the treatment of patients with chronic myeloid leukemia who are resistant or intolerant to imatinib.

Definition

Dasatinib monohydrate is a hydrate that is the monohydrate of dasatinib. It is used for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN; dasatinib monohydrate) as well as to anhydrous dasatinib (INN). It has a role as an antineoplastic agent and a tyrosine kinase inhibitor. It contains a dasatinib (anhydrous).

brand name

Sprycel (Bristol-Myers Squibb).

Biological Activity

chronic myeloid leukemia (cml) is a disease characterized by the presence of the philadelphia (ph+) chromosome and its oncogenic product, bcr-abl, that is present in >90% of the patients. dasatinib (bms-354825) is a novel, potent, and multitargeted kinase inhibitor that targets abl, src, kit, pdgfr, and other tyrosine kinases.

Synthesis

1-(2-Hydroxyethyl)piperazine

103-76-4

N-(2-Chloro-6-methylphenyl)-2-[(6-chloro-2-methyl-4-pyrimidinyl)amino]-5-thiazolecarboxamide

302964-08-5

Dasatinib monohydrate

863127-77-9

General procedure: to a mixture of N-(2-chloro-6-methylphenyl)-2-[(6-chloro-2-methyl-4-pyrimidinyl)amino]-5-thiazolecarboxamide (4.00 g, 10.14 mmol) and N-hydroxyethylpiperazine (6.60 g, 50.69 mmol) in n-butanol (40 mL) was added N,N-diisopropylethylamine (DIPEA, 3.53 mL, 20.26 mmol). The reaction mixture was heated with stirring at 118 °C for 4.5 h, followed by slow cooling to room temperature. The precipitated solid was collected by vacuum filtration and washed with n-butanol (5 mL) and subsequently dried. The crude product (5.11 g) was dissolved in hot 80% ethanol-water (80 mL) and the solution was clarified by filtration. The hot filtrate was slowly diluted with water (15 mL) and slowly cooled to room temperature. The precipitated solid was collected by vacuum filtration, washed with 50% ethanol-water (5 mL) and dried to afford N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)-1-piperazinyl)-2-methyl-4-pyrimidinyl)amino)-5-thiazolecarboxamide hydrate 4.27 g in 83.2% yield.1H NMR (400 MHz, DMSO -d6) δ 2.23 (s, 3H), 2.40 (s, 3H), 2.42 (t, 2H, J = 6 Hz), 2.48 (t, 4H, J = 6.3 Hz), 3.50 (m, 4H), 3.53 (q, 2H, J = 6 Hz), 4.45 (t, 1H, J = 5.3 Hz), 6.04 (s, 1H), 7.25 (t, 1H , J = 7.6 Hz), 7.27 (dd, 1H, J = 7.6, 1.7 Hz), 7.40 (dd, 1H, J = 7.6, 1.7 Hz), 8.21 (s, 1H), 9.87 (s, 1H), 11.47 (s, 1H).

in vitro

dasatinib is a potent atp-competitive inhibitor in biochemical assays with broad-spectrum antiproliferative activities against hematological and solid tumor cell lines. dasatinib was more potent than imatinib at inhibiting nonmutated bcr-abl kinase activity. in addition, the kinase activity of 14 out of 15 different clinically relevant, imatinib-resistant bcr-abl isoforms was successfully inhibited [1].

in vivo

mice were dosed with dasatinib or vehicle alone by gavage for 2 weeks, beginning 3 days after injection of ba/f3 cells. all vehicle-treated mice developed progressive disease. in contrast, dasatinib–treated mice harboring nonmutant bcr-abl or the clinically common imatinib-resistant mutation m351t appeared healthy with no evidence of weight loss, lethargy, or ruffled fur and showed more than one log lower levels of bioluminescent activity after 2 weeks of therapy [2].

IC 50

0.55 and 3.0 nm for src and bcr-abl tyrosine kinases, respectively

References

[1] shah np, tran c, lee fy, chen p, norris d, sawyers cl. overriding imatinib resistance with a novel abl kinase inhibitor. science. 2004 jul 16;305(5682):399-401.
[2] monika conchon, carla maria boquimpani de moura freitas, maria aparecida do carmo rego, and josé wilson ramos braga junior. dasatinib -

302962-49-8
863127-77-9
Synthesis of Dasatinib monohydrate from Dasatinib
Global Suppliers ( 474)
Supplier Tel Email Country ProdList Advantage
Nanjing EnMing Pharmaceutical Technology Co., Ltd. 13305188663 njempt@163.com China 16 58
Guangzhou Isun Pharmaceutical Co., Ltd 020-39119399 18927568969 isunpharm@qq.com China 4773 55
Guangzhou Tomums Life Science Co., Ltd. 020-31155029 18902330969 sales@tomums.cn China 4688 58
Sichuan Mingjian Pharmaceutical Chemical Co., Ltd. 15281098982 sales@mjpharma.cn China 57 58
Shanghai Boyle Chemical Co., Ltd. sales@boylechem.com China 2915 55
INTATRADE GmbH +49 3493/605464 sales@intatrade.de Germany 3563 66
3B Pharmachem (Wuhan) International Co.,Ltd. 18930552037 3bsc@sina.com China 15813 69
future industrial shanghai co., ltd 400-0066400 13621662912 sales@jonln.com China 1989 65
Chembest Research Laboratories Limited 021-20908456 sales@BioChemBest.com China 5996 61
Energy Chemical 400-0056266 sales8178@energy-chemical.com China 44850 61

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Dasatinib monohydrate pictures 2026-09-15 Dasatinib monohydrate
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0.99 RongNa Biotechnology Co.,Ltd
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1KG 98%min 30tons/month WUHAN FORTUNA CHEMICAL CO., LTD
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Dasatinib monohydrate Spectrum

Dasatinib R BMS-354825 Monohydrate N-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide hydrate Dasatinib monohydrate N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide monohydrate Dasatinib monohydrate, >=99% dasatinib monohydrate 5-Thiazolecarboxamide, N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-, hydrate (1:1) n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2- mmbf Dasatinib(TINIBS) Bms 35482503 Dasatinib hydrate Unii-rbz1571X5h n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide CS-295 Dasatinib(Sprycel) N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide,hydrate asatinib monohydrate Dasatinib monohydrate USP/EP/BP DasatinibmonohydrateDasatinib Dasatinib Monohydrate (BMS354825 Dasatinib Monohydrate intermediate Dashatini monohydrate Dasatinib (monohydrate) (Dasatinib Impurity) Dashatinib monohydrate Dasatinib monohydrate, 10 mM in DMSO Dasatinib monohydrate - Bio-X ? Dastinib n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide monohydrate Sprycel 863127-77-9 863121-77-9 332781-69-2 C22H26CIN7O2SH2O C22H26ClN7O2SH2O Inhibitors API Anti-cancer&immunity Molecular Targeted Antineoplastic Pharmaceutical 863127-77-9 SPRYCEL