2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs Bcr-Abl
  4. GMB-805

GMB-805 是一种 BCR-Abl 靶向 PROTAC 降解剂，其在 K562 细胞中的 DC50 为 30 nM。GMB-805 对 K562 细胞具有强效抗增殖活性，在动物体内展现出显著的抗肿瘤活性，且安全性特征优良。GMB-805 可用于慢性髓系白血病的相关研究。

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GMB-805

GMB-805 Chemical Structure

CAS No. : 2489876-41-5

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GMB-805 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Abl Bcr-Abl

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GMB-805 is a BCR-Abl PROTAC degrader with a DC50 of 30 nM in K562 cells. GMB-805 exerts antiproliferative activity in K562 cells. GMB-805 exhibits potent anti-tumor activity with favorable safety profile in vivo. GMB-805 can be used for chronic myeloid leukemia research[1][2].

IC50 & Target[1]

Bcr-Abl

30 nM (DC50)

体外研究
(In Vitro)

GMB-805 (1-30000 nM， 24 小时) 在 K562 细胞中剂量依赖性地降解 BCR/Abl 蛋白，其 DC50 为 30 nM[1]。
GMB-805 (1 μM， 8 小时) 在 K562 细胞中通过蛋白酶体诱导 BCR/Abl 蛋白降解[1]。
GMB-805 (1000 nM， 24 小时) 在 K562 细胞中降低 VHL 依赖性的 BCR/Abl 和 c-Abl 蛋白水平[1]。
GMB-805 (3 天) 对 BCR-Abl 驱动的 K562 细胞系具有强效抗增殖活性，其 IC50 为 169 nM[1]。

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

GMB-805 相关抗体:

Western Blot Analysis[1]

Cell Line: K562 cells
Concentration: 25, 250 and 2500 nM
Incubation Time: 24 h
Result: Demonstrated an enhanced ability to induce BCR-Abl degradation.

Western Blot Analysis[1]

Cell Line: K562 cells
Concentration: 1 μM
Incubation Time: 8 h
Result: Reduced BCR-Abl and Abl protein expression, and this effect was rescued by cotreatment with Epoxomicn (1 μM) (HY-13821).
Reduced BCR-Abl and Abl protein expression, and this effect was not rescued by cotreatment with Chloroquine (50 μM) (HY-17589A).
Reduced BCR-Abl and Abl protein expression, and this effect was rescued by cotreatment with Pevonedistat (1 μM) (HY-70062).
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Mice[1] 10 mg/kg i.p. T1/2 3.67 h
Mice[1] 10 mg/kg i.p. Tmax 2.00 h
Mice[1] 10 mg/kg i.p. Cmax 536 ng/mL
Mice[1] 10 mg/kg i.p. AUClast 2419 ng·h/mL
体内研究
(In Vivo)

GMB-805 (200 mg/kg，腹腔注射，每日一次，持续 3 天) 在 K562 异种移植小鼠模型中展现出强效的抗肿瘤活性，并且安全性良好[1]。

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

Animal Model: K562 cells induced-athymic mice[1]
Dosage: 200 mg/kg
Administration: i.p., once a day for 3 days
Result: Showed no significant increase in tumor volume.
No toxicity or weight loss was observed in the treated animals.
分子量

894.39

Formula

C42H46ClF2N9O7S
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

GMB-805 相关分类

  • 摩尔计算器

  • 稀释计算器

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

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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.

Keywords:

GMB-8052489876-41-5GMB805GMB 805PROTACsBcr-AblPROTACK562 cellssafety profileChronic Myeloid LeukemiaInhibitorinhibitorinhibit

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产品名称：
GMB-805
目录号：
HY-180968
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