1. GPCR/G Protein MAPK/ERK Pathway Apoptosis
  2. Ras Apoptosis
  3. TH-Z835

TH-Z835 is a mutant selective KRAS (G12D) inhibitor with an IC50 of 1.6 μM. TH-Z835 inhibits both mantGMPPNP/GPPNP exchange and GPPNP/mantGMPPNP exchange.

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

TH-Z835 Chemical Structure

TH-Z835 Chemical Structure

CAS No. : 2766209-50-9

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Based on 1 publication(s) in Google Scholar

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Description

TH-Z835 is a mutant selective KRAS (G12D) inhibitor with an IC50 of 1.6 μM. TH-Z835 inhibits both mantGMPPNP/GPPNP exchange and GPPNP/mantGMPPNP exchange[1].

IC50 & Target[1]

KRAS(G12D)

1.6 μM (IC50)

In Vitro

TH-Z835 reduces the pERK level in PANC-1 cells with an IC50 value less than 2.5 μM[1].
TH-Z835 conferres anti-proliferative effects, reduces the pERK and pAKT levels and induces apoptosis in other non-G12D mutant cancer cell lines, including 4T1 (KRAS(WT)), MIA PaCa-2 (KRAS(G12C)), CFPAC-1 (KRAS(G12V)), and HCT116 (KRAS(G13D)) cells, suggesting off-target effects[1].

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

In Vivo

TH-Z835 (10 mg/kg; ip) reduces the tumor volumes in the C57BL/6 mice model. TH-Z835 induces apoptosis and inhibits MAPK signaling in vivo[1].

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

Molecular Weight

498.66

Formula

C30H38N6O

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CN(CCC1)[C@@H]1COC2=NC(N3C[C@H]4N[C@H](CC4)C3)=C5C(CN(C6=CC=CC7=C6C(C)=CC=C7)CC5)=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 7.14 mg/mL (14.32 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 2.0054 mL 10.0269 mL 20.0537 mL
5 mM 0.4011 mL 2.0054 mL 4.0107 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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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 2.0054 mL 10.0269 mL 20.0537 mL 50.1344 mL
5 mM 0.4011 mL 2.0054 mL 4.0107 mL 10.0269 mL
10 mM 0.2005 mL 1.0027 mL 2.0054 mL 5.0134 mL
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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.

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Product Name:
TH-Z835
Cat. No.:
HY-146243
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