上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
PROTAC SOS1 degrader-1
PROTAC SOS1degrader-1 是一种有效的 PROTAC SOS1 激动剂，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。
PROTAC SOS1 degrader-1 Chemical Structure
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 agonist 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].
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IC50 & Target |
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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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
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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].
Shanghai Jinpan Biotech Co Ltd 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. |
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| 分子量 |
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| Formula |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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