2. TGF-beta/Smad
  3. TGF-β Receptor
  4. Fidrisertib

Fidrisertib  (Synonyms: BLU-782; IPN-60130; ALK2-IN-1)

目录号: HY-117887
产品使用指南 技术支持

Fidrisertib (BLU-782) 是口服有效的激活素受体样激酶 (ALK) 的抑制剂，可抑制 ALK2R206H、ALK2、ALK1、ALK6、ALK3、ALK4、TGFβR2 和 ALK5，IC50 分别为 0.2、0.6、3、24、45、65、67 和 155 nM。

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Fidrisertib Chemical Structure

Fidrisertib Chemical Structure

CAS No. : 2141955-96-4

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规格 价格 是否有货
5 mg ￥2200
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10 mg ￥3500
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Customer Review

Fidrisertib 相关抗体

Top Publications Citing Use of Products

查看 TGF-β Receptor 亚型特异性产品:

查看所有亚型
ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Fidrisertib (BLU-782) is the orally active inhibitor for activin receptor-like kinase 2 (ALK2) that inhibits ALK2R206H, ALK2, ALK1, ALK6, ALK3, ALK4, TGFβR2 and ALK5 with IC50s of 0.2, 0.6, 3, 24, 45, 65, 67 and 155 nM, respectively[1][2].

IC50 & Target

ALK2 R206H

0.2 nM (IC50)

ALK2

0.6 nM (IC50)

ALK1

3 nM (IC50)

ALK6

24 nM (IC50)

ALK4

65 nM (IC50)

TGF-βR2

67 nM (IC50)

ALK5

155 nM (IC50)

ACVR2A

9096 nM (IC50)

体外研究
(In Vitro)

Fidrisertib 在 HEK293T/ALK3KO 细胞中抑制 ALK2R206H 的活性，IC50 为 7 nM[2]。
Fidrisertib 阻断由 BMP 和促活素等配体激活的信号通路，降低 SMAD1 的磷酸化，从而抑制异位骨化[2]。

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

Fidrisertib 相关抗体:
体内研究
(In Vivo)

Fidrisertib（50 mg/kg，口服或腹腔注射，每日一次，连用 3-7 天）可防止小鼠肌肉损伤和骨折后的异位骨化，促进肌肉修复和骨骼愈合，且无明显毒性[2]。

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

Animal Model: ALK2R206H knock-in mouse model[2]
Dosage: 50 mg/kg
Administration: po or ip, once daily for 3-7 days
Result: Prevented heterotopic ossification after muscle injury (pinch injury) and fracture (fibular osteotomy).
Exhibited normal muscle repair response after muscle injury and normal healing after fracture.
Clinical Trial
分子量

562.70

同用名

BLU-782; IPN-60130; ALK2-IN-1

Formula

C31H42N6O4
CAS 号
性状

固体

颜色

Yellow to brown

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

Fidrisertib 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

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.

Keywords:

Fidrisertib2141955-96-4BLU-782 IPN-60130 ALK2-IN-1BLU782BLU 782IPN60130IPN 60130IPN-60130TGF-β ReceptorTransforming growth factor beta receptorsorally activeHEK293Inhibitorinhibitorinhibit

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