1. Protein Tyrosine Kinase/RTK
  2. Ephrin Receptor
  3. BT5528

BT5528 

目录号: HY-148101
产品使用指南

BT5528 是一种双环肽毒素结合物,一种 EphA2 激活剂。BT5528 由双环肽和 Auristatin E (HY-15582) 组成,是 BCY6099 的衍生物。BT5528 在大鼠模型中显示出强大的抗肿瘤活性,不导致出血或引起凝血毒性。

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BT5528 Chemical Structure

BT5528 Chemical Structure

CAS No. : 2648849-70-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BT5528 is a bicyclic peptide toxin conjugate, an EphA2 activator. BT5528 is made up of a bicyclic peptide and Auristatin E (HY-15582), is derivated from BCY6099. BT5528 shows potent anti-tumor activity without bleeding or coagulation toxicity in rats model[1][2].

IC50 & Target

EC50: 41.9 nM (EphA2)[1]

体外研究
(In Vitro)

BT5528 shows high affinity on EphA2 with a Kb value of 19.1 nM, and activates EphA2 in EphA2-expressing cells with a EC50 value of 41.9 nM[1].
BT5528 inhibits cancer cells growth with IC50s of 21.9 nM (HT-1080), 5.2 nM (PC-3), 21.6 nM (NCI-H1975), respectively[1].

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

体内研究
(In Vivo)

BT5528 (1, 2, 3 mg/kg; i.v.; once a week; 2-5 weeks) inhibits tumor growth in vivo in mice xenograft model[1].
BT5528 (3 mg/kg; i.v.; once a week; 3 weeks) exhibits greate ability to penetrate solid tumours in Non-small-cell lung carcinoma (NSCLC) Patient-derived xenograft (PDX) xenograft model in mice[1].

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

Animal Model: Xenograft model in mice with NCI-H1975 Non-small cell lung cancer, MDA-MB-231 Triple-negative breast cancer, MOLP-8 Multiple Myeloma[1]
Dosage: 1, 2, 3 mg/kg
Administration: Intravenous injection; once a week; for 5, 3, 2 weeks respectively
Result: Showed target-mediated efficacy in the high EphA2-expressing NCI-H1975 NSCLC xenograft and MDA-MB-231 TNBC xenograft, but there were no significant effects in the low EphA2-expressing MOLP-8 Multiple Myeloma xenograft.
Animal Model: Non-small-cell lung carcinoma (NSCLC) Patient-derived xenograft (PDX) xenograft model in mice[1]
Dosage: 3 mg/kg; compared with MEDI 547 (3 mg/kg)
Administration: Intravenous injection; once a week; for 3-4 weeks
Result: Maintained efficacy during 3 weeks, while MEDI-547 fails to show efficacy.
Didn’t affect D-Dimer, APTT or liver enzyme parameters.
分子量

4403.14

Formula

C201H315N53O52S3

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
  • 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

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目录号:
HY-148101
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