2. PROTAC MAPK/ERK Pathway GPCR/G Protein
  3. PROTACs Ras
  4. PROTAC SOS1 degrader-1

PROTAC SOS1degrader-1 是一种有效的 PROTAC SOS1 降解剂，DC50 为 98.4 nM。PROTAC SOS1 Degrader-1 在各种 KRAS 突变的癌细胞中显示出抗增殖活性。PROTAC SOS1 Degrader-1 具有抗肿瘤作用，且具有低毒性。

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PROTAC SOS1 degrader-1 Chemical Structure

PROTAC SOS1 degrader-1 Chemical Structure

CAS No. : 2913185-35-8

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1 mg ￥5500
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PROTAC SOS1 degrader-1 的其他形式现货产品:

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Other Forms of PROTAC SOS1 degrader-1:

PROTAC SOS1 degrader-1 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

PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity[1].

IC50 & Target

DC50: 98.4 nM (SOS1)[1]
体外研究
(In Vitro)

PROTAC SOS1 degrader-1 (compound 9d) (0.1, 1 μM) shows SOSI degradation activity with an SOS1 protein degradation of 56.2 and 92.5% at 0.1 and 1 μM, respectively[1].
PROTAC SOS1 degrader-1 (0-2000 nM; 24 h) exhibits SOS1 degradation activity with an DC50 of 98.4 nM in a dose- and time-dependent manner in NCI-H358 cells[1].
PROTAC SOS1 degrader-1 (0-2500 nM; 24 h) dose-dependently reduced the SOS1 protein level but showed no effect on SOS2 and KRAS up to 2.5 μM in NCI-H358 and AsPc-1 cells[1].
PROTAC SOS1 degrader-1 (0-2000 nM; 24 h) reduces the expression of KRAS-GTP, induced ERK phosphorylation with an IC50value of 72.3 nM, and significantly increases the pERK level after 6-24 h[1].

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

PROTAC SOS1 degrader-1 相关抗体:

Western Blot Analysis[1]

Cell Line: NCI-H358 cells
Concentration: 0-2000 nM
Incubation Time: 0-24 h
Result: Decreased the expression of SOS1 in a dose- and time-dependent manner in NCI-H358 cells.

RT-PCR[1]

Cell Line: NCI-H358 cells
Concentration: 1 µM
Incubation Time: 24, 48, 72 h
Result: Showed no effffect on SOS2 mRNA expression.

Cell Proliferation Assay[1]

Cell Line: NCI-H358, MIA-PaCa2, AsPC-1, SK-LU-1, SW620, A549 cells
Concentration: 0-10000 nM
Incubation Time: 7 days
Result: Showed anti-proliferation activity with an IC50s of 0.525, 0.218, 0.307, 0.115, 0.199, 0.232 µM and DC50s of 0.098, 0.255, 0.119, 0.104, 0.125, 0.022 µM for NCI-H358, MIA-PaCa2, AsPC-1, SK-LU-1, SW620, A549 cells, respectively.
体内研究
(In Vivo)

PROTAC SOS1 degrader-1 (10 mg/kg; i.p.) shows good PK profile with low toxicity[1].
PROTAC SOS1 degrader-1 (0, 10, 20 mg/kg; i.p.; once a day for 3 weeks) shows significant anti-tumor activities in the xenograft mouse model[1].
Pharmacokinetic Parameters of PROTAC SOS1 degrader-1 in BALB/c mice[1].

compound dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUClast (h*ng/mL) AUCINF (h*ng/mL) MRTINF-obs(h)
9d 10 8.64±0.31 0.250v±0 1221±132 3895±335 4420±363 10.2±0.4
Male BALB/c mice; 10 mg/kg for i.p.[1].

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

Animal Model: Male BALB/c mice[1]
Dosage: 10 mg/kg (dissolved in solution containing dimethyl sulfoxide, PEG400, and 10% hydroxypropyl-β-cyclodextrin in water (5/5/90, v/v/v))
Administration: I.p.
Result: Showed good PK profile with high exposure (AUC0‑∞ = 4420 h*ng/mL) and maximum concentration (Cmax = 1221 ng/mL) in mouse plasma.
Animal Model: 6-8 weeks, BALB/c mice [1]
Dosage: 0, 10, 20 mg/kg
Administration: I.p.; once a day for a week
Result: Showed low toxicity for mouse.
Animal Model: 6-8 weeks, BALB/c nude mice (NCI-H358 tumor xenografts) [1]
Dosage: 0, 10, 20 mg/kg
Administration: I.p.; once a day for 3 weeks;
Result: Inhibited the tumor growth by 72.5 and 86.1% at 10 and 20 mg/kg, respectively.
Animal Model: 6-8 weeks, BALB/c nude mice (NCI-H358 tumor xenografts)[1]
Dosage: 0, 20, 50 mg/kg
Administration: Intratumoral injection; twice-weekly for 5 weeks
Result: Significantly prevented tumor growth in vivo with a good safety profile.
分子量

1051.79

Formula

C57H76ClFN10O4S
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 SOS1 degrader-1 相关分类

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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:

PROTAC SOS1 degrader-12913185-35-8PROTACsRaslow toxicityanti-tumorNCI-H358 cellsanti-proliferationKRAS-GTPpERKxenografts modelKRAS MutationsInhibitorinhibitorinhibit

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