2. Membrane Transporter/Ion Channel Cell Cycle/DNA Damage
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  4. QBS10072S dihydrochloride

QBS10072S dihydrochloride 是一种能穿透血脑屏障 (BBB) 的双功能化疗剂，包含一个 LAT1 靶向域和细胞毒性域。QBS10072S dihydrochloride 对 LAT1 介导的底物摄取的抑制效力 (IC50 = 21 μM) 比对 LAT2 (IC50 = 1100 μM) 高约 50 倍。QBS10072S dihydrochloride 通过 LAT1 介导的主动转运进入表达 LAT1 的肿瘤细胞，能够引起 DNA 链间交联，导致 DNA 损伤和细胞死亡。QBS10072S dihydrochloride 可用于胶质母细胞瘤及侵袭性 T 细胞淋巴瘤的研究。

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QBS10072S dihydrochloride

QBS10072S dihydrochloride Chemical Structure

CAS No. : 1802735-31-4

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QBS10072S dihydrochloride 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

QBS10072S dihydrochloride is a bifunctional chemotherapeutic agent that can cross the blood-brain barrier (BBB), comprising a LAT1-targeting domain and a cytotoxic domain. QBS10072S dihydrochloride exhibits inhibitory potency against LAT1-mediated substrate uptake (IC50 = 21 μM) of approximately 50-fold higher than that against LAT2 (IC50 = 1100 μM). QBS10072S dihydrochloride enters LAT1-expressing tumor cells via LAT1-mediated active transport, induces DNA interstrand crosslinking, and causes DNA damage and cell death. QBS10072S dihydrochloride can be used for the research of glioblastoma and aggressive T-cell lymphoma[1][2].

体外研究
(In Vitro)

QBS10072S (30 分钟) dihydrochloride 可诱导胶质母细胞瘤 (GBM) 细胞系 (U251、LN229、8MGBA、42MGBA、DBTRG、AM38) 出现剂量依赖性的活力丧失，其 EC50 值范围为 5.0 至 40 μM[1]。
QBS10072S (16 小时) dihydrochloride 可在 U251 和 LN229 胶质母细胞瘤 (GBM) 细胞中诱导呈剂量依赖性的 DNA 损伤，但处理 16 小时后对正常人星形胶质细胞 (NHA) 无该作用[1]。
QBS10072S (1 周) dihydrochloride 可在 LAT1 阳性的 H9、HH、MJ 和 Hut78 T 细胞淋巴瘤细胞系中诱导剂量依赖性的存活率降低，其 IC50 值范围为 4.4 μM (Hut78) 至 51 μM (HH)[2]。

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

QBS10072S dihydrochloride 相关抗体:
体内研究
(In Vivo)

QBS10072S (10 mg/kg；静脉注射；每周 1 次；持续 4-6 周) dihydrochloride 可抑制 U251 GBM 肿瘤生长[1]。
QBS10072S (2-8 mg/kg；静脉注射；每两周 1 次；共给药 3 次) dihydrochloride 可抑制 LN229 胶质母细胞瘤 (GBM) 的肿瘤生长[1]。
QBS10072S (8 mg/kg) dihydrochloride 在 H9T 细胞淋巴瘤异种异植小鼠模型中可产生显著的抗肿瘤作用[2]。

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

Animal Model: athymic nu/nu (female, 5 weeks old, intracranially injected with luciferase-expressing U251 human GBM cells)[1]
Dosage: 10 mg/kg
Administration: i.v.; once weekly; 4 and 6 weeks
Result: Achieved 95% tumor growth inhibition (TGI) at Day 35 and extended median survival from 37 days (vehicle) to 70 days with 10 mg/kg weekly for 6 weeks.
Achieved 86% TGI at Day 35 and extended median survival to 45 days with 10 mg/kg weekly for 4 weeks.
Animal Model: athymic nu/nu (female, 5 weeks old, intracranially injected with luciferase-expressing LN229 human GBM cells)[1]
Dosage: 2, 4 and 8 mg/kg
Administration: i.v.; once every two weeks; three total doses
Result: Induced dose-dependent tumor growth inhibition: 72% TGI at 2 mg/kg, 73% at 4 mg/kg, and 84% at 8 mg/kg at Day 53; extended median survival from 56 days (vehicle) to 66.5 days (2 mg/kg), 71 days (4 mg/kg), and 74 days (8 mg/kg).
分子量

406.18

Formula

C15H24Cl4N2O2
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

QBS10072S dihydrochloride 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

QBS10072S1802735-31-4EAATDNA/RNA SynthesisDNA Alkylator/CrosslinkerExcitatory amino acid transporter Glutamate transporter| L-type amino acid transporter 1glioblastomaALK-negative anaplastic large cell lymphomaSèzary syndromeT-cell lymphomaperipheral T-cell lymphoma not otherwise specifiedangioimmunoblastic T-cell lymphomaLAT1LAT2SLC7A5Inhibitorinhibitorinhibit

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