2. GPCR/G Protein MAPK/ERK Pathway
  3. SOS1 Ras
  4. SOS1-IN-15

SOS1-IN-15 (Compound 37) is an orally active SOS1 inhibitor with an IC50 of 5 nM. SOS1-IN-15 is a promising agent candidate for the research of KRAS-driven cancer.

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SOS1-IN-15

SOS1-IN-15 構造式

CAS 番号 : 2793404-47-2

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
5 mg $400 在庫あり
10 mg $650 在庫あり
25 mg $1250 在庫あり
50 mg $1900 在庫あり
100 mg $2800 在庫あり
200 mg   お問い合わせ  
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SOS1-IN-15 関連抗体

Top Publications Citing Use of Products

Ras アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
K-Ras H-Ras N-Ras Ras

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製品説明

SOS1-IN-15 (Compound 37) is an orally active SOS1 inhibitor with an IC50 of 5 nM. SOS1-IN-15 is a promising agent candidate for the research of KRAS-driven cancer[1].

IC50 & Target[1]

SOS1

5 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
MIA PaCa-2 IC50
178 nM
Compound: 8
Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
[PMID: 37778239]
体外実験

SOS1-IN-15 (Compound 37) (0.1 nM-0.1 mM; 72 h) displays prominent inhibitory activities in Mia-paca-2 cancer cells (IC50 = 178 ± 42 nM)[1].
SOS1-IN-15 has a limited inhibition of CYP and hERG[1].

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

SOS1-IN-15 関連抗体

Cell Proliferation Assay[1]

Cell Line: Mia-paca-2 pancreas cancer cells
Concentration: 0.1 nM-0.1 mM
Incubation Time: 72 h
Result: Inhibited the proliferation with an IC50 of 178 ± 42 nM.
体内実験

SOS1-IN-15 (Compound 37) (50 mg/kg; p.o.; daily for 22 days) inhibits tumor volume in mice[1].

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

Animal Model: BALB/c nude mice bearing Mia-paca-2 pancreas tumors[1]
Dosage: 50 mg/kg
Administration: Oral administration, daily for 22 days
Result: Showed 49% tumor inhibition. No animal mortality and significant difference in the mice’s body weight were observed during the study period.
Animal Model: Male CD-1 Mice[1]
Dosage: 20 mg/kg
Administration: Oral administration (Pharmacokinetic Analysis)
Result: In Vivo Pharmacokinetic Properties of the Compounds in Male CD-1 Micea
T1/2 (h) Tmax (h) Cmax (ng/mL) AUC (ng⋅h/mL) MRT (h) Kel (h-1)
SOS1-IN-15 11.4 3.67 1550 9900 4.19 0.25

aCompounds (20 mg/kg) were P.O. dosed in a mixture of 63% water + 30% PEG +5 % DMSO + 2% Tween 80 in male ICR mice (n = 3). Abbreviations: T1/2, elimination half-life; Tmax, plasma peak time after administration; Cmax, maximum plasma concentration; AUC, area under concentration-time curve. MRT, mean residence time; Kel, elimination rate constant.
分子量

536.55

分子式

C28H27F3N6O2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

N#CC1(CC1)C(N2CCN3C4=CC5=C(C=C4OC[C@H]3C2)N=C(C)N=C5N[C@H](C)C6=CC=CC(C(F)F)=C6F)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMF : ≥ 100 mg/mL (186.38 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8638 mL 9.3188 mL 18.6376 mL
5 mM 0.3728 mL 1.8638 mL 3.7275 mL
10 mM 0.1864 mL 0.9319 mL 1.8638 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

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In Vivo Dissolution Calculator
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純度とドキュメンテーション

純度: 98.04%

COA (251 KB) HNMR (376 KB) LCMS (114 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMF 1 mM 1.8638 mL 9.3188 mL 18.6376 mL 46.5940 mL
5 mM 0.3728 mL 1.8638 mL 3.7275 mL 9.3188 mL
10 mM 0.1864 mL 0.9319 mL 1.8638 mL 4.6594 mL
15 mM 0.1243 mL 0.6213 mL 1.2425 mL 3.1063 mL
20 mM 0.0932 mL 0.4659 mL 0.9319 mL 2.3297 mL
25 mM 0.0746 mL 0.3728 mL 0.7455 mL 1.8638 mL
30 mM 0.0621 mL 0.3106 mL 0.6213 mL 1.5531 mL
40 mM 0.0466 mL 0.2330 mL 0.4659 mL 1.1648 mL
50 mM 0.0373 mL 0.1864 mL 0.3728 mL 0.9319 mL
60 mM 0.0311 mL 0.1553 mL 0.3106 mL 0.7766 mL
80 mM 0.0233 mL 0.1165 mL 0.2330 mL 0.5824 mL
100 mM 0.0186 mL 0.0932 mL 0.1864 mL 0.4659 mL
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SOS1-IN-15 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

SOS1-IN-152793404-47-2SOS1RasRas/Rac guanine nucleotide exchange factor 1orally activeKRAS-driven cancerMia-paca-2BALB/c nude miceInhibitorinhibitorinhibit

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製品番号:
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