Dasatinib hydrochloride 达沙替尼盐酸盐; BMS-354825 hydrochloride|cas:854001-07-3|西域试剂

Dasatinib hydrochloride 达沙替尼盐酸盐; BMS-354825 hydrochloride,98.86%

产品编号：Bellancom-10181A| CAS NO：854001-07-3| 分子式：C₂₂H₂₇Cl₂N₇O₂S| 分子量：524.47

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货号	价格	库存与货期
Bellancom-10181A	￥880.00	杭州北京（现货）
Bellancom-10181A	￥1200.00	杭州北京（现货）
Bellancom-10181A	￥1650.00	杭州北京（现货）
Bellancom-10181A	￥2400.00	杭州北京（现货）

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Dasatinib hydrochloride 达沙替尼盐酸盐; BMS-354825 hydrochloride

产品介绍

Dasatinib (BMS-354825) hydrochloride 是一种具有口服活性的，ATP 竞争性的，双重 Src/Bcr-Abl 抑制剂，具有有效的抗肿瘤活性。对 Src 和 Bcr-Abl 的 K_i 值分别为 16 pM 和 30 pM。Dasatinib hydrochloride 抑制 Bcr-Abl 和 Src 的IC₅₀ 分别为 <1.0 nM 和 0.5 nM。Dasatinib hydrochloride 还诱导凋亡 (apoptosis) 和自噬 (autophagy)。

生物活性

Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The K_is are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC₅₀s of <1.0 nM and 0.5 nM, respectively. Dasatinib hydrochloride also induces apoptosis and autophagy.

体外研究

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.
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 (t_1/2s) of 3.3 and 3.1 h for i.v. and oral, respectively. The oral bioavailability (F_po) in this study is 27%.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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:	C_max of 13.2 and 0.5 μM for i.v. and oral, respectively.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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:	C_max of 13.2 and 0.5 μM for i.v. and oral, respectively.

性状

Solid

溶解性数据

In Vitro:

DMSO : 15 mg/mL (28.60 mM; Need ultrasonic and warming)

H₂O : 10 mg/mL (19.07 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9067 mL	9.5334 mL	19.0669 mL
5 mM	0.3813 mL	1.9067 mL	3.8134 mL
10 mM	0.1907 mL	0.9533 mL	1.9067 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制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

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 3.33 mg/mL (6.35 mM); Clear solution

此方案可获得 ≥ 3.33 mg/mL (6.35 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 33.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 3.33 mg/mL (6.35 mM); Clear solution

此方案可获得 ≥ 3.33 mg/mL (6.35 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 33.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 3.33 mg/mL (6.35 mM); Clear solution

此方案可获得 ≥ 3.33 mg/mL (6.35 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 33.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。