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Cat. No.: HY-183365

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SL43

SL43 is an orally active and potent SOS1 inhibitor with a K_d of 0.16 μM. SL43 disrupts SOS1-KRAS interaction, inhibits SOS1-mediated nucleotide exchange on KRAS mutants, and suppresses RAS-MAPK signaling. SL43 exerts antiproliferative activity against KRAS-mutant cancer cells, induces early apoptosis and G1 phase cell cycle arrest, and reduces phosphorylated MEK and ERK levels. SL43 suppresses tumor growth in a colorectal cancer xenograft model.

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화학식: C₂₇H₃₃ClN₄
분자량:449.03

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

SL43 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

K-RAS

All Ras Isoforms :

All p38 MAPK Isoforms :

All ERK Isoforms :

All MEK Isoforms :

In Vitro

SL43 binds to SOScat with a K_d of 0.16 μM, indicating high affinity for the SOS1 catalytic domain^[1].
SL43 potently disrupts the SOS1-KRAS^G12C interaction with an IC₅₀ of 13.0 nM^[1].
SL43 preferentially inhibits SOS1-mediated nucleotide exchange on KRAS^G12C, KRAS^G12V, and KRAS^G12D mutants with IC₅₀ values ranging from 13.4-29.1 nM, while showing weaker inhibition of KRAS^WT (IC₅₀ = 95.8 nM)^[1].
SL43 (120 h) potently and selectively inhibits the proliferation of KRAS-mutant CRC cell lines (IC₅₀ = 0.028-0.238 μM) with over 100-fold selectivity over KRAS wild-type CRC cell lines (IC₅₀ = 2.495-4.520 μM)^[1].
SL43 (10-40 nM; 72 h) dose-dependently suppresses colony formation in SW620 and HCT116 KRAS-mutant CRC cell lines^[1].
SL43 (200-800 nM; 48 h) dose-dependently induces early apoptosis and G1 phase cell cycle arrest in SW620 and HCT116 KRAS-mutant CRC cell lines^[1].
SL43 (50-200 nM; 48 h) dose-dependently inhibits the RAS-MAPK signaling pathway in SW620 and HCT116 KRAS^G12D/G13D CRC cell lines by reducing phosphorylated MEK and ERK levels^[1].

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

Apoptosis Analysis^[1]

Cell Line:

KRAS-mutant CRC cell lines (SW620/G12V, HCT116/G13D)
Concentration:

200, 400, 800 nM
Incubation Time:

48 h
Result:

Significantly increased the proportion of early apoptotic cells, with high-concentration groups reaching 35.47% in SW620 cells and 25.97% in HCT116 cells.

Cell Cycle Analysis^[1]

Cell Line:

KRAS-mutant CRC cell lines (SW620/G12V, HCT116/G13D)
Concentration:

200, 400, 800 nM
Incubation Time:

48 h
Result:

Induced dose-dependent G₁ phase cell cycle arrest, with the G₁ population increasing from 64.13% to 78.04% in SW620 cells and from 35.34% to 57.59% in HCT116 cells.

Western Blot Analysis^[1]

Cell Line:

KRAS-mutant CRC cell lines (SW620/G12V, HCT116/G13D)
Concentration:

50, 100, 200 nM
Incubation Time:

48 h
Result:

Led to a concentration-dependent decrease in p-MEK and p-ERK levels in both SW620 and HCT116 cells.
Left total MEK and ERK expression unaltered.

Parmacokinetics

Species	Dose	Route	AUC_0-t	T_max	T_1/2	C_max	F
Mice^[1]	20 mg/kg	i.v.	6504.1 ng·h/mL	0.1 h	4.2 h	3649.1 ng/mL	/
Mice^[1]	20 mg/kg	p.o.	3697.2 ng·h/mL	2.0 h	4.6 h	468.2 ng/mL	56.8 %

In Vivo

SL43 (20-40 mg/kg; i.g.; daily; 18 days) exerts potent dose-dependent antitumor efficacy in KRAS-mutant colorectal cancer xenografts, achieving a maximum TGI of 74.9% at 40 mg/kg with no detectable systemic toxicity^[1].
SL43 (400-800 mg/kg; p.o.; single dose) has a favorable safety profile in BALB/c mice, with an estimated oral median lethal dose (LD₅₀) exceeding 800 mg/kg^[1].

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

Animal Model:

Colorectal cancer BALB/c nude mice (female, 6-8 weeks old, 20-22 g, subcutaneous inoculation of HCT116 KRASG13D cells)^[1]
Dosage:

20 mg/kg; 40 mg/kg
Administration:

p.o.; daily; 18 days
Result:

Produced a tumor growth inhibition (TGI) rate of 57.2% at 20 mg/kg.
Produced a tumor growth inhibition (TGI) rate of 74.9% at 40 mg/kg.
Induced no significant body weight loss or observable histological alterations in major organs (heart, liver, spleen, lungs, kidneys) at either dose.

Chemical Information

분자량 449.03
화학식 C₂₇H₃₃ClN₄
SMILES

ClC1=CC=C([C@@H](C)NC2=NC(NCC(C)(C)C)=NC3=CC=C(C4=CCCCC4)C=C23)C=C1
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Liu X, et al. Discovery of a potent and orally available SOS1 inhibitor with antitumor efficacy in KRAS-mutant colorectal cancers. Bioorg Chem. 2026;175:109823. [Content Brief]

Calculators

몰농도 계산기

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

Mass Mass

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Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
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수량:
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SL43

All Ras Isoforms

All p38 MAPK Isoforms

All ERK Isoforms

All MEK Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

SL43 Related Classifications

HY-183365 Related Classifications