2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. SOS1-IN-14

SOS1-IN-14 is a potent, selective and orally active SOS1 inhibitor with an IC50 value of 3.9 nM. SOS1-IN-14 can be absorbed in the intestine via a P-glycoprotein-mediated efflux mechanism. SOS1-IN-14 can be used to research KRAS-mutated cancers. SOS1-IN-14 has better potent tumor suppression than BI-3406 (HY-125817).

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

SOS1-IN-14 Chemical Structure

SOS1-IN-14 Chemical Structure

CAS No. : 2793405-20-4

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 671 In-stock
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10 mM * 1 mL in DMSO USD 671 In-stock
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25 mg USD 1900 In-stock
50 mg USD 3050 In-stock
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Based on 1 publication(s) in Google Scholar

SOS1-IN-14 Related Antibodies

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Description

SOS1-IN-14 is a potent, selective and orally active SOS1 inhibitor with an IC50 value of 3.9 nM. SOS1-IN-14 can be absorbed in the intestine via a P-glycoprotein-mediated efflux mechanism. SOS1-IN-14 can be used to research KRAS-mutated cancers. SOS1-IN-14 has better potent tumor suppression than BI-3406 (HY-125817)[1].

IC50 & Target

IC50: 3.9 nM (SOS1)[1]
In Vitro

SOS1-IN-14 (compound 13c) exhibits cellular SOS1 inhibition with an IC50 of 21 nM[1].
SOS1-IN-14 has certain inhibition for CYP2D6, CYP2C9, CYP2C8 and CYP3A4 with IC50s of 2.5 μM, 6.5 μM, 43.3 μM and 54.3 μM, respectively, indicating that it has a certain risk of drug-drug interaction[1].

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

SOS1-IN-14 Related Antibodies
In Vivo

SOS1-IN-14 (50 mg/kg; p.o.; qd) exhibits 83.0% tumor suppression in Mia-paca-2 pancreas xenograft mice tumor models[1].
SOS1-IN-14 shows a favorable pharmacokinetic profile with a bioavailability of 86.8% in beagles[1].
Pharmacokinetic Parameters of SOS1-IN-14 (compound 13c) in ICR mice, Sprague-Dawley rats and Beagle dogs[1].

ICR Mice Sprague–Dawley Rats Beagle Dogs
Administration p.o., 50 mg/kg i.v., 2 mg/kg p.o., 10 mg/kg i.v., 2 mg/kg p.o., 20 mg/kg
Tmax (h) 0.5 0.08 3 0.08 2
T1/2 (h) 4.61 1.17 2.32 3.83 6.68
Cmax (μg/mL) 2670 1261 265 568 1840
AUC0-24 (ng/mL·h) 32300 970 1683 2962 25725
CL (mL/min/kg) / 2068 / 11.3 /
Vss (L/kg) / 2126 / 3.88 /
F (%) / / 34.5 / 86.8
Kel (h-1) 0.265 / / / /
MRT (h) 4.67 / / / /

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

Animal Model: BALB/c nude mice (KRAS G12C variant Mia-paca-2 xenograft models)[1]
Dosage: 50 mg/kg
Administration: p.o.; q.d., for 21 days
Result: Exhibited 83.0% tumor suppression.
Showed better potent tumor suppression than BI-3406 (HY-125817).
Molecular Weight

550.57

Formula

C29H29F3N6O2
CAS No.
Appearance

Solid

Color

Light yellow to light brown

SMILES

N#CC1(C(N2C[C@]3([H])CCOC4=CC5=NC(C)=NC(N[C@@H](C6=CC=CC(C(F)F)=C6F)C)=C5C=C4N3CC2)=O)CC1
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 : 250 mg/mL (454.07 mM; Need ultrasonic; 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 1.8163 mL 9.0815 mL 18.1630 mL
5 mM 0.3633 mL 1.8163 mL 3.6326 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
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 1.8163 mL 9.0815 mL 18.1630 mL 45.4075 mL
5 mM 0.3633 mL 1.8163 mL 3.6326 mL 9.0815 mL
10 mM 0.1816 mL 0.9081 mL 1.8163 mL 4.5407 mL
15 mM 0.1211 mL 0.6054 mL 1.2109 mL 3.0272 mL
20 mM 0.0908 mL 0.4541 mL 0.9081 mL 2.2704 mL
25 mM 0.0727 mL 0.3633 mL 0.7265 mL 1.8163 mL
30 mM 0.0605 mL 0.3027 mL 0.6054 mL 1.5136 mL
40 mM 0.0454 mL 0.2270 mL 0.4541 mL 1.1352 mL
50 mM 0.0363 mL 0.1816 mL 0.3633 mL 0.9081 mL
60 mM 0.0303 mL 0.1514 mL 0.3027 mL 0.7568 mL
80 mM 0.0227 mL 0.1135 mL 0.2270 mL 0.5676 mL
100 mM 0.0182 mL 0.0908 mL 0.1816 mL 0.4541 mL
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SOS1-IN-14 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-142793405-20-4RasSOS1anticancerantitumorBI-340Mia-paca-2KRASG12CcarcinomaInhibitorinhibitorinhibit

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