2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs Anaplastic lymphoma kinase (ALK)
  4. PROTAC EML4-ALK Degrader-2

PROTAC EML4-ALK Degrader-2 is an EML4-ALK PROTAC degrader. PROTAC EML4-ALK Degrader-2 shows potent selective inhibitory activity to ALK with an IC50 of 1.6 nM. PROTAC EML4-ALK exhibits selectivity over IGF1R, INSR, FLT3, and FGFR2. PROTAC EML4-ALK Degrader-2 shows anti-cancer activities both in vitro and vivo. PROTAC EML4-ALK Degrader-2 can be used for non-small cell lung cancer (NSLC), liver lung and cervical cancer research.
(Pink: EML4-ALK ligand (HY-15656); Blue: Cereblon ligand (HY-10984); Black: linker (HY-42776)).

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

PROTAC EML4-ALK Degrader-2

PROTAC EML4-ALK Degrader-2 Chemical Structure

CAS No. : 2417174-28-6

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PROTAC EML4-ALK Degrader-2 Related Antibodies

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Description

PROTAC EML4-ALK Degrader-2 is an EML4-ALK PROTAC degrader. PROTAC EML4-ALK Degrader-2 shows potent selective inhibitory activity to ALK with an IC50 of 1.6 nM. PROTAC EML4-ALK exhibits selectivity over IGF1R, INSR, FLT3, and FGFR2. PROTAC EML4-ALK Degrader-2 shows anti-cancer activities both in vitro and vivo. PROTAC EML4-ALK Degrader-2 can be used for non-small cell lung cancer (NSLC), liver lung and cervical cancer research[1][2]. (Pink: EML4-ALK ligand (HY-15656); Blue: Cereblon ligand (HY-10984); Black: linker (HY-42776)).

IC50 & Target[1]

EML4-ALK

 

In Vitro

PROTAC EML4-ALK Degrader-2 (compound B3) (72 h) shows do not increase the toxicity to normal cells in normal human liver cell line LO2 and shows anti-proliferation effect in H3122, H2228, H1299. A549 and HeLa cells with IC50s of 0.3, 0.9, 2.84, 1.6 and 1.18 μM, respectively[1].
PROTAC EML4-ALK Degrader-2 (0-50 nM,0-32 h) decreases the cellular levels of ALK fusion proteins in a concentration-and time-dependent manner in H3122 cells[1].
PROTAC EML4-ALK Degrader-2 (10-500 nM) shows high selectivity to ALK, maintaining moderate inhibition activity to IGF1R and INSR, and not induce the degradation of IGF1R and INSR[1].
PROTAC EML4-ALK Degrader-2 is effective against ALK-resistant mutations, with its anti-resistance activity spectrum being limited to BaF3-ALK-L1196M and BaF3-ALK-G1202R cells, exhibiting marginally superior activity to LDK378 in targeting BaF3-ALK-L1196M cells [1].

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

PROTAC EML4-ALK Degrader-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: H3122 cells
Concentration: 0, 1, 5, 10, 20, 50 and 100 nM
Incubation Time: 0, 4, 8, 16, 24 and 32 h
Result: Degraded ALK in a dose dependent manner for 8 h; effectively degraded ALK at 50 nM for 8 h; degraded all the ALK protein at 200 nM.
Achieved amount (>80%) of EML4-ALK degradation after 16 h treatment at 100 nM.
Not observed maximum degradation of EML4-ALK degradation until 24 h at 100 nM.
Inhibited p-ALK and downregulated the level of p-STAT3 after 24 h at 100 nM.
Induced ALK degradation in a concentration dependent manner after 24 h.
Achieved maximum degradation of EML4-ALK degradation at 50 nM.
Downregulated the level of p-ALK and p-STAT3 in a concentration dependent manner after 24 h.
Parmacokinetics
Species Dose Route AUCall AUCinf T1/2 CL Vss
Rat[1] 1 mg/kg i.v. 1322 ng·h/mL 1409 ng·h/mL 4.09 h 16.3 mL/min/kg 1335 mL/kg
In Vivo

PROTAC EML4-ALK Degrader-2 (compound B3) (25-50 mg/kg, o.p., once daily for 15 days) inhibits growth of xenograft tumors in a dose-dependent manner with safety profile in H3122 xenograft mice[1].

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

Animal Model: H3122 cells (5 x 106) induced-female BALB/c nude mice (6-7 weeks) (18-22g) [1]
Dosage: 25, 50 mg/kg
Administration: o.p., once daily for 15 days
Result: Observed tumor growth inhibitions (TGIs) of 37% and 48% at dose of 25 mg/kg and 50 mg/kg, respectively.
Did not cause significant weight loss and toxicity.
Molecular Weight

1060.65

Formula

C52H66ClN9O11S
CAS No.
SMILES

O=C1NC(C(CC1)N2C(C3=C(C2=O)C(NCCOCCOCCOCCNC(CCN4CCC(CC4)C5=CC(OC(C)C)=C(NC6=NC=C(C(NC7=C(S(=O)(C(C)C)=O)C=CC=C7)=N6)Cl)C=C5C)=O)=CC=C3)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC EML4-ALK Degrader-2 Related Classifications

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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:

PROTAC EML4-ALK Degrader-22417174-28-6PROTACsAnaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246H3122 cellselectiveanti-proliferation effectnon-small cell lung cancercervical cancerInhibitorinhibitorinhibit

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