2. Protein Tyrosine Kinase/RTK
  3. TAM Receptor
  4. UNC9426

UNC9426 is a potent and selective TYRO3 inhibitor (IC50 = 2.1 nM), demonstrating 276-fold and 90-fold selectivity over MERTK and AXL, respectively. UNC9426 reduces platelet aggregation without increasing bleeding time and blocks TYRO3-dependent functions in tumor cells and macrophages. UNC9426 demonstrates a favorable safety profile with no significant increase in bleeding risk in vivo. UNC9426 can be used for functional studies of TYRO3-dependent phenotypes such as non-small cell lung cancer (NSCLC).

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UNC9426

UNC9426 Chemical Structure

CAS No. : 3051784-94-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

UNC9426 Related Antibodies

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Axl Mer Tyro3

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Description

UNC9426 is a potent and selective TYRO3 inhibitor (IC50 = 2.1 nM), demonstrating 276-fold and 90-fold selectivity over MERTK and AXL, respectively. UNC9426 reduces platelet aggregation without increasing bleeding time and blocks TYRO3-dependent functions in tumor cells and macrophages. UNC9426 demonstrates a favorable safety profile with no significant increase in bleeding risk in vivo. UNC9426 can be used for functional studies of TYRO3-dependent phenotypes such as non-small cell lung cancer (NSCLC)[1].

IC50 & Target[1]

Tyro3

2.1 nM (IC50)

Axl

190 nM (IC50)

MERTK

580 nM (IC50)

In Vitro

UNC9426 (compound 12) (0.5 nM-10 μM) exhibits differential binding potency against the three TAM kinase family members (TYRO3, MERTK, and AXL), as evidenced by its highest affinity for TYRO3 (EC50 = 89.8 nM)[1].
UNC9426 (10 μM, 10 min) inhibits human platelet aggregation and reduces the expression of human platelet surface activation markers PAC-1 and P-selectin[1].
UNC9426 (100-10000 nM, 0-10 h) significantly inhibits the efferocytosis activity in macrophages in THP1 cells[1].
UNC9426 (30-10000 nM, 7-10 days) exhibits potent inhibition of colony formation in NSCLC cell cultures with EC50 values of 170 nM (H1650) and 197 nM (H1975)[1].

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

UNC9426 Related Antibodies
In Vivo

UNC9426 (10 mg/kg, i.v.) does not cause significant bleeding side effects in C57BL/6 mice[1].

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

Animal Model: Wildtype C57BL/6 mice (6-12 weeks)[1]
Dosage: 10 mg/kg
Administration: i.v.
Result: Reduced the total bleeding duration and the time until initial cessation of bleeding in mice compared to the control.
Showed no significantly affect on the number of rebleeding events in mice during the 15-minute experimental period.
Molecular Weight

632.64

Formula

C32H34F6N6O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H](CC1)CC[C@@H]1N2C=C(C3=CC=C(C=C3)CN4CCN(CC4)C)C5=CN=C(N=C52)NC6=CC(C(F)(F)F)=CC(C(F)(F)F)=C6
Shipping

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 : 20.59 mg/mL (32.55 mM; ultrasonic and warming and heat to 60°C; 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 1.5807 mL 7.9034 mL 15.8068 mL
5 mM 0.3161 mL 1.5807 mL 3.1614 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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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 1.5807 mL 7.9034 mL 15.8068 mL 39.5169 mL
5 mM 0.3161 mL 1.5807 mL 3.1614 mL 7.9034 mL
10 mM 0.1581 mL 0.7903 mL 1.5807 mL 3.9517 mL
15 mM 0.1054 mL 0.5269 mL 1.0538 mL 2.6345 mL
20 mM 0.0790 mL 0.3952 mL 0.7903 mL 1.9758 mL
25 mM 0.0632 mL 0.3161 mL 0.6323 mL 1.5807 mL
30 mM 0.0527 mL 0.2634 mL 0.5269 mL 1.3172 mL
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UNC9426 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:

UNC94263051784-94-9UNC 9426UNC-9426TAM ReceptorTyro3AxlMerorally bioavailableTYRO3platelet aggregationTYRO3-dependent functionsmacrophagestumorTAM kinaseMERTKAXLNSCLCcolony formationC57BL/6 miceTHP1 cellsInhibitorinhibitorinhibit

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