Dasatinib monohydrate
Modify Date: 2024-01-02 19:41:30
Dasatinib monohydrate structure
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Common Name | Dasatinib monohydrate | ||
|---|---|---|---|---|
| CAS Number | 863127-77-9 | Molecular Weight | 506.021 | |
| Density | 1.408 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C22H28ClN7O3S | Melting Point | 97-99 °C(lit.) | |
| MSDS | N/A | Flash Point | N/A | |
Use of Dasatinib monohydrateDasatinib monohydrate (BMS-354825 monohydrate) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Ki values of 16 pM and 30 pM for Src and Bcr-Abl, respectively[1]. |
| Name | N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide,hydrate |
|---|---|
| Synonym | More Synonyms |
| Description | Dasatinib monohydrate (BMS-354825 monohydrate) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Ki values of 16 pM and 30 pM for Src and Bcr-Abl, respectively[1]. |
|---|---|
| Related Catalog | |
| Target |
Ki: 16 pM (Src), 30 pM (Bcr-Abl)[1] IC50: <1.0 (Bcr-Abl), 0.50 (Src), 0.40 (Lck), 0.50 (Yes), 5.0 (c-Kit), 28 (PDGFRβ), 100 (p38), 180 (Her1), 720 (Her2), 880 (FGFR-1), 1700 (MEK)[1] |
| In Vitro | Dasatinib demonstrates significant activity against Bcr-Abl, Src, Lck, Yes, c-Kit, PDGFRβ, p38, Her1, Her2, FGFR-1, and MEK with IC50s of <1.0, 0.50, 0.40, 0.50, 5.0, 28, 100, 180, 720, 880, and 1700 nM, respectively[1]. Dasatinib shows antiproliferative activities aversus K562 chronic myelogenous leukemia (CML), PC3 human prostate tumor, MDA-MB-231 human breast tumor, and WiDr human colon tumor cell lines with IC50s of <1.0 nM, 9.4 nM, 12 nM, and 52 nM, respectively[1]. |
| In Vivo | Dasatinib (5 mg/kg and 50 mg/kg, qd×10d, 5 on-2 off) possesses potent antitumor activity and a high safety margin in a K562 xenograft model of chronic myelogenous leukemia (CML), demonstrating complete tumor regressions and low toxicity at multiple dose levels[1]. Dasatinib (10 mg/kg) has a pharmacokinetic profile appropriate for continued advancement into in vivo efficacy studies. Dasatinib (10 mg/kg) demonstrates favorable half-lives (t1/2s) of 3.3 and 3.1 h for i.v. and oral, respectively. The oral bioavailability (Fpo) in this study is 27%[1]. Animal Model: Nude mice bearing K562 xenografts Dosage: 5 mg/kg and 50 mg/kg Administration: Oral administration on a 5 day on and 2 day off schedule. Result: Showed partial tumor regressions after one treatment cycle and complete disappearance of the tumor mass by the end of drug treatment. No toxicity (animal deaths, lack of weight gain) was observed. Animal Model: Sprague-Dawley Rats Dosage: 10 mg/kg (Pharmacokinetic Analysis) Administration: Oral and i.v. Result: Cmax of 13.2 and 0.5 μM for i.v. and oral, respectively. |
| References |
| Density | 1.408 g/cm3 |
|---|---|
| Melting Point | 97-99 °C(lit.) |
| Molecular Formula | C22H28ClN7O3S |
| Molecular Weight | 506.021 |
| Exact Mass | 505.166290 |
| PSA | 143.98000 |
| LogP | 3.39810 |
| Water Solubility | MAY DECOMPOSE |
| Hazard Codes | C,Xi |
|---|---|
| Risk Phrases | R34:Causes burns. R36/37/38:Irritating to eyes, respiratory system and skin . |
| Safety Phrases | S26-S27-S28-S36/37/39-S45 |
| RIDADR | UN 3263 8/PG 2 |
| WGK Germany | 3 |
| RTECS | QD8530000 |
| Packaging Group | II |
| Hazard Class | 4.3 |
|
~86%
Dasatinib monoh... CAS#:863127-77-9 |
| Literature: BRISTOL-MYERS SQUIBB COMPANY Patent: WO2005/77945 A2, 2005 ; Location in patent: Page/Page column 52 ; WO 2005/077945 A2 |
|
~%
Dasatinib monoh... CAS#:863127-77-9 |
| Literature: WO2005/77945 A2, ; Page/Page column 58-59 ; WO 2005/077945 A2 |
![N-(2-Chloro-6-methylphenyl)-2-[(6-chloro-2-methyl-4-pyrimidinyl)amino]-5-thiazolecarboxamide structure](https://www.chemsrc.com/caspic/159/302964-08-5.png)
| Dasatinib |
| SPRYCEL (TN) |
| Dasatinibmonohydrate |
| N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)-1-piperazinyl)-2-methyl-4-pyrimidinyl)amino)-1,3-thiazole-5-carboxamide monohydrate |
| 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 hydrate (1:1) |
| N-(2-chloro-6-methylphenyl)-2-(6-(4-(3-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-ylamino) thiazole-5-carboxamide monohydrate |
| cc-335 |
| Dasatinib hydrate |
| N-(2-Chloro-6-methylphenyl)-2-({6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl}amino)-1,3-thiazole-5-carboxamide hydrate (1:1) |
| 5-Thiazolecarboxamide, N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-, hydrate (1:1) |
| Dasatinib hydrate (JAN) |
| N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide monohydrate |
| Dasatinib monohydrate |
| dasatinib.H2O |
| MFCD08704581 |
- Shanghai Jizhi Biochemical Technology Co., Ltd
- China
- Product Name: Dasatinib monohydrate
- Price: ￥448.0/500mg ￥138.0/100mg
- Purity: 99.0%
- Stocking Period: Inquiry
- Contact: Liu jia
- DC Chemicals Limited
- China
- Product Name: Dasatinib monohydrate
- Price: $200.0/100mg $400.0/250mg $800.0/1g
- Purity: 98.0%
- Stocking Period: 3 Day
- Contact: Tony Cao
- Dayang Chem (Hangzhou) Co., Ltd.
- China
- Product Name: Dasatinib monohydrate
- Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
- Purity: 98.0%
- Stocking Period: Inquiry
- Contact: Ms Wang
- Henan Tianfu Chemical Co., Ltd.
- China
- Product Name: N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide,hydrate
- Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
- Purity: 99.0%
- Stocking Period: Inquiry
- Contact: Anson
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