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Cat. No.: HY-180172

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TRK-IN-33

TRK-IN-33 is a TRK inhibitor. TRK-IN-33 exhibits excellent TRKA^G667C degradation (DC₅₀ = 24.69 nM; D_max > 90%), while sparing the wild-type protein in virto. TRK-IN-33 shows antiproliferative activities against Ba/F3-LMNA-NTRK1^G667C cells with an IC₅₀ value of 2.48 nM. TRK-IN-33 effectively inhibits tumor growth and enhances apoptosis in tumor tissues with no apparent toxicity in vivio. TRK-IN-33 can be used for NTRK fusion−positive cancers research.

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화학식: C₂₂H₂₂ClFN₆O₃
분자량:472.90

보관:

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

Data Sheet (274 KB)

TRK-IN-33 Chemical Structure

사이즈

가격

재고

수량

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

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]

TrkA

All Trk Receptor Isoforms :

In Vitro

TRK-IN-33 (compound 20) (0.1-10 μM) exhibits excellent degradation efficiency against TRKA^G667C resistant mutation (degradation = -1.16% at 0.1 μM, degradation = 69.30% at 1 μM, degradation = 68.75% at 10 μM) and inhibitory activities with IC₅₀ = 23.8 nM in Ba/F3-LMNA-NTRK1^WT cells.^[1].
TRK-IN-33 (0.1-10 μM, 24 h) displays favorable dose-dependent degradation on TRKA G667C mutant protein in Ba/F3-LMNA-NTRK1^G667C cells^[1].
TRK-IN-33 (1 μM) exhibits superior pharmacokinetic properties in CD-1 mice, SD rats, or humans microsomes with T_1/2 = 24.8, 53.8 and 57.1min; C_Lint = 0.0683, 0.0599 and 0.0230 mL/min/mg, respectively^[1].

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

Cell Viability Assay^[1]

Cell Line:

Ba/F3-LMNA-NTRK1^G667C cells
Concentration:

0.1, 1 and 10 μM
Incubation Time:

24 h
Result:

Exhibited > 90% maximal degradation, potentially overcoming on-target resistance in TRKA G667C resistant mutation.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	CL	MRT_0-t	MRT_0-∞	F
Mice^[1]	1 mg/kg	i.v.	0.249 h	0.083 h	590 ng/mL	231 ng·h/mL	232 ng·h/mL	442 mL/h/kg	0.268 h	0.275 h	/
Mice^[1]	10 mg/kg	p.o.	0.437 h	0.500 h	754 ng/mL	930 ng·h/mL	932 ng·h/mL	4313 mL/h/kg	0.903 h	0.911 h	40.2 %

In Vivo

TRK-IN-33 (compound 20) (30 or 50 mg.kg, i.p., twice daily for 28 consecutive days) overcomes TRK resistance driven by the G667C mutation with good tolerability and safety profile in the Ba/F3-LMNA-NTRK1^G667C mice xenograft model^[1].

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

Animal Model:

Ba/F3-LMNA-NTRK1 sup>G667C cells (3 × 10⁶) induced-female BALB/c nude mice (18-22 g, 4 weeks old)^[1]
Dosage:

30 or 50 mg/kg
Administration:

i.p., twice daily for 28 consecutive days
Result:

Significantly inhibited tumor growth in a dose-dependent manner, with inhibition rates of 71.65 and 80.38% at 30 and 50 mg/kg, respectively.
Observed no statistically significant changes in body weight.
Revealed no apparent damage in major organs, including the heart, liver, spleen, lung, and kidney.
Revealed g a significant reduction of TRK fluorescence intensity.
Suppressed tumor cell proliferation and enhanced apoptosis in tumor tissues.

Chemical Information

분자량 472.90
화학식 C₂₂H₂₂ClFN₆O₃
SMILES

FC1=C(NC(C2=NN(C(C)C)C(N)=C2C(N)=O)=O)C=C(NC(CC3=CC=C(Cl)C=C3)=O)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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Song J, et al. Discovery of Novel Bifunctional Agents as Potent TRK Inhibitors and Degraders against xDFG Mutation Resistance. J Med Chem. 2025 Dec 25;68(24):26383-26404. [Content Brief]

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

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.

Keywords

MOQ

Minimum order quantity

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:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

TRK-IN-33

All Trk Receptor Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

TRK-IN-33 Related Classifications

HY-180172 Related Classifications