2. PROTAC Protein Tyrosine Kinase/RTK Apoptosis
  3. PROTACs ROS Kinase Apoptosis
  4. SIA​​IS039

SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker).

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SIA​​IS039 Chemical Structure

SIA​​IS039 Chemical Structure

CAS No. : 2570251-69-1

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Based on 1 publication(s) in Google Scholar

SIA​​IS039 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker)[1].

IC50 & Target[1]

Cereblon

 

Molecular Weight

878.40

Formula

C46H53ClN9O5P
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C(N(CC1=C2C=CC=C1C#CCCCN3CCN(C4CCN(C5=CC=C(NC6=NC=C(Cl)C(NC7=CC=CC=C7P(C)(C)=O)=N6)C(OC)=C5)CC4)CC3)C2=O)CC8)NC8=O
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Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (113.84 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 1.1384 mL 5.6922 mL 11.3843 mL
5 mM 0.2277 mL 1.1384 mL 2.2769 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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In Vivo Dissolution Calculator
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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 1.1384 mL 5.6922 mL 11.3843 mL 28.4608 mL
5 mM 0.2277 mL 1.1384 mL 2.2769 mL 5.6922 mL
10 mM 0.1138 mL 0.5692 mL 1.1384 mL 2.8461 mL
15 mM 0.0759 mL 0.3795 mL 0.7590 mL 1.8974 mL
20 mM 0.0569 mL 0.2846 mL 0.5692 mL 1.4230 mL
25 mM 0.0455 mL 0.2277 mL 0.4554 mL 1.1384 mL
30 mM 0.0379 mL 0.1897 mL 0.3795 mL 0.9487 mL
40 mM 0.0285 mL 0.1423 mL 0.2846 mL 0.7115 mL
50 mM 0.0228 mL 0.1138 mL 0.2277 mL 0.5692 mL
60 mM 0.0190 mL 0.0949 mL 0.1897 mL 0.4743 mL
80 mM 0.0142 mL 0.0712 mL 0.1423 mL 0.3558 mL
100 mM 0.0114 mL 0.0569 mL 0.1138 mL 0.2846 mL
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SIA​​IS039 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:

SIA​​IS0392570251-69-1PROTACsROS KinaseApoptosisc-ros oncogene 1ROS1HCC78Ba/F3CD74-ROS1SDC4-ROS1proteasomal degradation SLC34A2-ROS1proliferationcycle arrestclonogenicityInhibitorinhibitorinhibit

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HY-159147
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