2. GPCR/G Protein MAPK/ERK Pathway
  3. 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.

For research use only. We do not sell to patients.

SOS1-IN-15 Chemical Structure

SOS1-IN-15 Chemical Structure

CAS No. : 2793404-47-2

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Based on 1 publication(s) in Google Scholar

SOS1-IN-15 Related Antibodies

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Description

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)

In Vitro

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 Related Antibodies

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.
In Vivo

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.
Molecular Weight

536.55

Formula

C28H27F3N6O2
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (9.32 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
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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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation
References

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
DMSO 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
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SOS1-IN-15 Related Classifications

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-152793404-47-2Rasorally activeKRAS-driven cancerMia-paca-2BALB/c nude miceInhibitorinhibitorinhibit

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