2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. RTx-303

RTx-303 是一种口服有效的选择性 DNA 聚合酶 θ (Polθ) 抑制剂 (IC50 = 5.1 nM)。RTx-303 具有显著的细胞活性，并能显著增强 PARP 抑制剂在 BRCA1/2 突变细胞和患者来源的异种移植模型中的活性。RTx-303 可用于 BRCA2 突变型乳腺癌的研究。

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RTx-303

RTx-303 Chemical Structure

CAS No. : 3035072-99-9

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RTx-303 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RTx-303 is an orally active, selective DNA polymerase θ (Polθ) inhibitor (IC50 = 5.1 nM). RTx-303 exhibits significantly high cellular potency and strongly potentiates PARPi in BRCA1/2 mutant cells and patient-derived xenograft models. RTx-303 can be used for the study of BRCA2-mutated breast cancer[1].

产品应用

1. 该化合物可作为示踪剂。
2. 该化合物可作为 NMR、GC-MS 或 LC-MS 分析中的内标品，用于定量分析。
体外研究
(In Vitro)

RTx-303 可显著抑制 Polθ-pol 的活性，但对其他 DNA 聚合酶 (如 Polβ、Polη、Polγ 等) 无显著影响[1]。
RTx-303 (10 μM) 对大多数激酶无显著抑制作用 (活性抑制率 > 90%) ，仅对少数激酶有轻微抑制作用，例如 PASK (活性抑制率 75%) 和 ATR/ATRIP (活性抑制率 77%) [1]。
RTx-303 对 HRD 细胞 (HCT116 BRCA2-/-) 的 IC50 为 81.2 nM，对 HR 功能正常的细胞 (HCT116 BRCA2+/+) 的 IC50 > 1280 nM，表明其选择性 >100 倍[1]。
RTx-303 (5 μM，5 天) 与奥拉帕尼 (HY-10162) 联合使用可显著降低 ID8 BRCA2-/-细胞的 IC50 (从 2 μM 降至 0.12 μM)，并恢复 PARPi 耐药细胞对奥拉帕尼的敏感性[1]。

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

RTx-303 相关抗体:
体内研究
(In Vivo)

RTx-303 (60 mg/kg，口服，每日两次，疗程 28-42 天) 无论单独使用还是与 PARP 抑制剂联合使用，均能有效抑制小鼠模型中 BRCA2 突变肿瘤的生长，且未观察到明显的体重减轻，表明其安全性良好[1]。
RTx-303 (60 mg/kg，口服，每日两次，疗程 56 天) 与奥拉帕尼联合使用，可预防 MDA-MB-436 荷瘤小鼠 BRCA1 突变肿瘤对 PARP 抑制剂的获得性耐药[1]。

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

Animal Model: For the BR-05-0566 (BR-05-0568) BRCA2 mutant PDX study, ∼ 30 mm3 tumor fragment was implanted subcutaneously into female BALB/c mice 6-8 weeks old[1].
Dosage: 60 mg/kg
Administration: P.o., twice daily for 28 days (BR-05-0566) to 42 days (BR-05-0568)
Result: BR-05-0566 model: Significantly inhibited tumor growth (compared to the vehicle group); combined with olaparib, it led to tumor regression; tumor volume reduction >80% in the combination group.
BR-05-0568 model: Combined with talazoparib, it resulted in 100% complete tumor elimination.
No significant weight loss was observed in any group.
Animal Model: 10 × 106 MDA-MB-436 (bearing BRCA1-Mutant) cells were injected with Matrigel subcutaneously into female BALB/c mice, 6-8 weeks old[1].
Dosage: 60 mg/kg
Administration: P.o., twice daily for 56 days
Result: Treated with Olaparib, tumors regressed rapidly and there was no recurrence.
分子量

569.49

Formula

C24H22D3F7N4O4
CAS 号
非标记 CAS
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

RTx-303 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

RTx-3033035072-99-9RTx303RTx 303DNA/RNA SynthesisDNA polymerase thetaPolθBRCA mutant tumorsBreast cancerPatient-derived xenograftPDXCell-derived xenograftCDXInhibitorinhibitorinhibit

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