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  3. Dasatinib (GMP Like)

Dasatinib (GMP Like)  (Synonyms: BMS-354825 (GMP Like))

目录号: HY-10181GL
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Dasatinib (GMP Like) (BMS-354825 (GMP Like)) 是 GMP Like 级别的 Dasatinib (HY-10181)。GMP Like 级别的小分子可用做细胞疗法中的辅助试剂。Dasatinib (BMS-354825) 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 SrcBcr-AblKi 值分别为 16 pM 和 30 pM。Dasatinib 抑制 Bcr-AblSrcIC50 分别为 <1.0 nM 和 0.5 nM。Dasatinib 还诱导凋亡 (apoptosis) 和自噬 (autophagy)。

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Dasatinib (GMP Like)

Dasatinib (GMP Like) Chemical Structure

CAS No. : 302962-49-8

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  • 生物活性

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生物活性

Dasatinib (GMP Like) (BMS-354825 (GMP Like)) is Dasatinib (HY-10181) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively[1]. Dasatinib also induces apoptosis and autophagy.

体外研究
(In Vitro)

Dasatinib (GMP Like) 对 Bcr-Abl、Src、Lck、Yes、c-Kit、PDGFRβ、p38、Her1、Her2、FGFR-1 和 MEK 具有显著活性,IC50<1.0、0.50、分别为 0.40、0.50、5.0、28、100、180、720、880 和 1700 nM[1]
与 K562 慢性粒细胞白血病 (CML)、PC3 相比,Dasatinib (GMP Like) 显示出抗增殖活性人前列腺肿瘤、MDA-MB-231 人乳腺肿瘤和 WiDr 人结肠肿瘤细胞系,IC50 分别为 <1.0 nM、9.4 nM、12 nM 和 52 nM[1]

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

体内研究
(In Vivo)

Dasatinib (GMP Like) (5 mg/kg 和 50 mg/kg,qd×10d,5 on-2 off) 在慢性粒细胞白血病 (CML) 的 K562 异种移植模型中具有有效的抗肿瘤活性和高安全边际,表明肿瘤完全消退且低多剂量水平的毒性[1]
Dasatinib (GMP Like) (10 mg/kg) 的药代动力学特征适合继续推进体内药效研究。Dasatinib (GMP Like) (10 mg/kg) 在静脉注射和口服时表现出良好的半衰期 (t1/2s),分别为 3.3 和 3.1 小时。本研究口服生物利用度 (Fpo) 为 27%[1]

MCE 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.
分子量

488.01

Formula

C22H26ClN7O2S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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