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 화학구조

CAS No. : 3051784-94-9

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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UNC9426 Related Antibodies

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Axl Mer Tyro3

  • Biological Activity

  • 순도&문서

  • References

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제품 설명

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
Parmacokinetics
Species Dose Route T1/2 Cmax AUClast Vss CL F
Mice 3 mg/kg i.v. 10.0 h 3.4 μM 18.7 μM·h 2.6 L/kg 3.5 mL/min/kg /
Mice 3 mg/kg p.o. 9.4 h 0.35 μM 6.76 μM·h / / 36 %
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.
분자량

632.64

화학식

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
선적

Room temperature in continental US; may vary elsewhere.
보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
용액&용해도
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.

  • 몰농도 계산기

  • 농도 희석 계산기

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
순도&문서
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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상품명:
UNC9426
Cat. No.:
HY-173268
수량:
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