2. GPCR/G Protein MAPK/ERK Pathway Apoptosis
  3. Ras Apoptosis
  4. KRAS G12D inhibitor 14

KRAS G12D inhibitor 14 is a potent KRAS G12D inhibitor with a KD of 33 nM for binding to KRAS G12D protein. KRAS G12D inhibitor 14 decreases the active form of KRAS G12D (KRAS G12D-GTP) but not KRAS G13D.

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KRAS G12D inhibitor 14 Chemical Structure

KRAS G12D inhibitor 14 Chemical Structure

CAS No. : 2765254-39-3

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Description

KRAS G12D inhibitor 14 is a potent KRAS G12D inhibitor with a KD of 33 nM for binding to KRAS G12D protein. KRAS G12D inhibitor 14 decreases the active form of KRAS G12D (KRAS G12D-GTP) but not KRAS G13D[1].

IC50 & Target[1]

KRas G12D

33 nM (Kd)

In Vitro

KRAS G12D inhibitor 14 (compound KD-8) shows antiproliferative activity with an IC50 of 2.1 μM against three KRAS G12D-mutated cells (Panc1, SW1990 and CT26). KRAS G12D inhibitor 14 decreases the active form of KRAS (KRAS-GTP) in KRAS G12D mutated cancer cell lines (CT26 and SW1990) but not in KRAS G13D mutated cancer cell lines (HCT116). KD-8 also causes efficient apoptosis of SW1990 and CT26 cancer cells. KRAS G12D inhibitor 14 down-regulates the phosphorylated Raf and Erk in CT26 and SW1990 cancer cell lines but not in HeLa cells (KRAS WT)[1].

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

KRAS G12D inhibitor 14 Related Antibodies
In Vivo

KRAS G12D inhibitor 14 (compound KD-8) (40 mg/kg or 60 mg/kg; i.p.) exhibits significant antitumor efficacy in a CT26 tumor model with a tumor growth inhibition (TGI) of 42% or 53% without causing apparent toxicity[1].

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

420.45

Formula

C20H19F3N4OS
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

COC1=CC=C(C=C1C2=CC3=C(N=CN=C3S2)N4CC5CCC4CN5)C(F)(F)F
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 : 50 mg/mL (118.92 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 2.3784 mL 11.8920 mL 23.7840 mL
5 mM 0.4757 mL 2.3784 mL 4.7568 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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Calculation results:
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 2.3784 mL 11.8920 mL 23.7840 mL 59.4601 mL
5 mM 0.4757 mL 2.3784 mL 4.7568 mL 11.8920 mL
10 mM 0.2378 mL 1.1892 mL 2.3784 mL 5.9460 mL
15 mM 0.1586 mL 0.7928 mL 1.5856 mL 3.9640 mL
20 mM 0.1189 mL 0.5946 mL 1.1892 mL 2.9730 mL
25 mM 0.0951 mL 0.4757 mL 0.9514 mL 2.3784 mL
30 mM 0.0793 mL 0.3964 mL 0.7928 mL 1.9820 mL
40 mM 0.0595 mL 0.2973 mL 0.5946 mL 1.4865 mL
50 mM 0.0476 mL 0.2378 mL 0.4757 mL 1.1892 mL
60 mM 0.0396 mL 0.1982 mL 0.3964 mL 0.9910 mL
80 mM 0.0297 mL 0.1487 mL 0.2973 mL 0.7433 mL
100 mM 0.0238 mL 0.1189 mL 0.2378 mL 0.5946 mL
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KRAS G12D inhibitor 14 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:

KRAS G12D inhibitor 142765254-39-3RasApoptosisantiproliferativeKRAS G12DKRAS-GTPPanc1SW1990CT26 cellsInhibitorinhibitorinhibit

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