2. PROTAC MAPK/ERK Pathway GPCR/G Protein
  3. PROTACs Ras
  4. PROTAC pan-KRAS degrader-1

PROTAC pan-KRAS degrader-1 是一种 pan-KRAS PROTAC 降解剂，可降解多种 KRAS 突变体，例如 G12D、G12C、G12V 和 G13D。PROTAC pan-KRAS degrader-1 可强效降解 AGS 细胞中的 KRAS 突变 (G12D)，DC50 为 1.1 nM，Dmax 为 95%。PROTAC pan-KRAS degrader-1 可用于研究由 KRAS 突变或扩增引起的疾病，尤其是乳腺癌、膀胱癌、胃癌等癌症。粉色：pan-KRAS ligand (HY-176490)；蓝色：VHL ligase ligand (HY-170353)；黑色：linker (HY-176491)；

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PROTAC pan-KRAS degrader-1 Chemical Structure

PROTAC pan-KRAS degrader-1 Chemical Structure

CAS No. : 3043908-63-7

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PROTAC pan-KRAS degrader-1 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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K-Ras H-Ras N-Ras Ras

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC pan-KRAS degrader-1 is a pan-KRAS PROTAC degrader for degrading different KRAS mutation types, such as G12D, G12C, G12V, and G13D. PROTAC pan-KRAS degrader-1 potently degrades KRAS mutation (G12D) in AGS cells, with a DC50 of 1.1 nM, Dmax of 95%. PROTAC pan-KRAS degrader-1 can be used to search diseases caused by KRAS mutation or amplification, especially cancers such as breast cancer, bladder cancer, gastric cancer, etc[1]. Pink: pan-KRAS ligand (HY-176490); Blue: VHL ligase ligand (HY-170353); Black: linker (HY-176491);

IC50 & Target

KRas G12D

1.1 nM (DC50)

KRas G12D

3 nM (IC50)

KRAS(G12C)

5 nM (IC50)

KRas G12V

10 nM (IC50)

KRas G12D

2.6 nM (IC50)

KRAS G13D

13 nM (IC50)

体外研究
(In Vitro)

PROTAC pan-KRAS degrader-1 (Compound 144) (0.31-20000 nM，96 小时) 显著抑制 AGS、SW620、AsPC-1、H358、HCT116 和 MKN-1 细胞中不同 KRAS 突变类型的细胞增殖，其 IC50 分别为 3、10、2.6、5、13 和 0.9 nM[1]。
PROTAC pan-KRAS degrader-1 (1.53-100000 nM) 可强效降解 AGS 细胞中的 KRAS 突变 (G12D)，DC50 为 1.1 nM，Dmax 为 95%[1]。
PROTAC pan-KRAS degrader-1 (0.16-100 nM，24 h) 能有效降解 AGS 和 SW620 细胞中的不同KRAS突变(G12D和G12V)，最大降解效率分别在 0.8 和 4 nM[1]。

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

PROTAC pan-KRAS degrader-1 相关抗体:

Cell Proliferation Assay[1]

Cell Line: AGS, SW620, AsPC-1, H358, HCT116, MKN-1 cells
Concentration: 0.31, 1.22, 4.88, 19.53, 78.13, 312.5, 1250, 5000, 20000 nM
Incubation Time: 96 h
Result: Significantly inhibited cell proliferation with different KRAS mutation types in AGS (G12D), SW620 (G12V), AsPC-1 (G12D), H358 (G12C), HCT116 (G13D), MKN-1 cells (WT amp), with IC50 s of 3, 10, 2.6, 5, 13, and 0.9 nM, respectively.

Western Blot Analysis[1]

Cell Line: AGS, SW620 cells
Concentration: 0.16, 0.8, 4, 20, 100 nM
Incubation Time: 24 h
Result: Potently degraded different KRAS mutation (G12D and G12V) in AGS and SW620 cells, and the maximum degradation efficacy at 0.8 and 4 nM, respectively.
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Dog 1 mg/kg i.v. CL 6.19 mL/min/kg
Dog 1 mg/kg i.v. T1/2 20.5 hr
Dog 1 mg/kg i.v. Vss 3.46 L/kg
Dog 1 mg/kg i.v. AUClast 2522 ng·h/mL
Dog 1 mg/kg i.v. C0 9889 ng/mL
分子量

1192.38

Formula

C63H71F2N13O7S
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

PROTAC pan-KRAS degrader-1 相关分类

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  • 稀释计算器

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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:

PROTAC pan-KRAS degrader-13043908-63-7PROTACsRasPROTACDegradationPan-KRASG12DG12CG12Vand G13DCancerInhibitorinhibitorinhibit

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目录号：
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